6WH4

Crystal structure of HTR2A with inverse agonist

External Resource: Annotation

Domain Annotation: SCOP2 Classification
Domain Annotation: ECOD Classification
Protein Family Annotation
Gene Ontology: Gene Product Annotation
InterPro: Protein Family Classification
Pharos: Disease Associations
Membrane Protein Annotation: OPM
Membrane Protein Annotation: PDBTM
Membrane Protein Annotation: MemProtMD
Membrane Protein Annotation: mpstruc

Domain Annotation: SCOP2 Classification SCOP2 Database Homepage

Chains	Type	Family Name	Domain Identifier	Family Identifier	Provenance Source (Version)
A	SCOP2B Superfamily	G protein-coupled receptor-like	8091246	3000473	SCOP2B (2022-06-29)
A	SCOP2B Superfamily	G protein-coupled receptor-like	8091246	3000473	SCOP2B (2022-06-29)
A	SCOP2B Superfamily	Cytochromes	8057879	3001526	SCOP2B (2022-06-29)
B	SCOP2B Superfamily	G protein-coupled receptor-like	8091246	3000473	SCOP2B (2022-06-29)
B	SCOP2B Superfamily	G protein-coupled receptor-like	8091246	3000473	SCOP2B (2022-06-29)
C	SCOP2B Superfamily	G protein-coupled receptor-like	8091246	3000473	SCOP2B (2022-06-29)
C	SCOP2B Superfamily	Cytochromes	8057879	3001526	SCOP2B (2022-06-29)
C	SCOP2B Superfamily	G protein-coupled receptor-like	8091246	3000473	SCOP2B (2022-06-29)

Domain Annotation: ECOD Classification ECOD Database Homepage

Chains	Family Name	Domain Identifier	Architecture	Possible Homology	Homology	Topology	Family	Provenance Source (Version)
A	7tm_1_2	e6wh4A2	A: alpha bundles	X: Family A G protein-coupled receptor-like (From Topology)	H: Family A G protein-coupled receptor-like (From Topology)	T: Family A G protein-coupled receptor-like	F: 7tm_1_2	ECOD (1.6)
A	Cytochrom_B562_1	e6wh4A1	A: alpha bundles	X: Four-helical up-and-down bundle	H: Cytochromes (From Topology)	T: Cytochromes	F: Cytochrom_B562_1	ECOD (1.6)
B	7tm_1_2	e6wh4B2	A: alpha bundles	X: Family A G protein-coupled receptor-like (From Topology)	H: Family A G protein-coupled receptor-like (From Topology)	T: Family A G protein-coupled receptor-like	F: 7tm_1_2	ECOD (1.6)
B	Cytochrom_B562_1	e6wh4B1	A: alpha bundles	X: Four-helical up-and-down bundle	H: Cytochromes (From Topology)	T: Cytochromes	F: Cytochrom_B562_1	ECOD (1.6)
C	7tm_1_2	e6wh4C2	A: alpha bundles	X: Family A G protein-coupled receptor-like (From Topology)	H: Family A G protein-coupled receptor-like (From Topology)	T: Family A G protein-coupled receptor-like	F: 7tm_1_2	ECOD (1.6)
C	Cytochrom_B562_1	e6wh4C1	A: alpha bundles	X: Four-helical up-and-down bundle	H: Cytochromes (From Topology)	T: Cytochromes	F: Cytochrom_B562_1	ECOD (1.6)

Protein Family Annotation Pfam Database Homepage

Chains	Accession	Name	Description	Comments	Source
A, B, C	PF07361	Cytochrome b562 (Cytochrom_B562)	Cytochrome b562	-	Family
A, B, C	PF00001	7 transmembrane receptor (rhodopsin family) (7tm_1)	7 transmembrane receptor (rhodopsin family)	-	Family

Gene Ontology: Gene Product Annotation Gene Ontology Database Homepage

Chains	Polymer	Molecular Function	Biological Process	Cellular Component
A, B, C	5-hydroxytryptamine receptor 2A,Soluble cytochrome b562 fusion	protein tyrosine kinase activator activity enzyme regulator activity kinase activator activity enzyme activator activity molecular function activator activity molecular function regulator activity protein kinase activator activity protein kinase regulator activity kinase regulator activity neurotransmitter receptor activity molecular transducer activity signaling receptor activity G protein-coupled amine receptor activity G protein-coupled serotonin receptor activity protein tyrosine kinase activator activity enzyme regulator activity kinase activator activity enzyme activator activity molecular function activator activity molecular function regulator activity protein kinase activator activity protein kinase regulator activity kinase regulator activity neurotransmitter receptor activity molecular transducer activity signaling receptor activity G protein-coupled amine receptor activity G protein-coupled serotonin receptor activity G protein-coupled receptor activity transmembrane signaling receptor activity Gq/11-coupled serotonin receptor activity protein-containing complex binding binding identical protein binding protein binding cation binding ion binding serotonin binding organic cyclic compound binding amine binding heterocyclic compound binding small molecule binding virus receptor activity exogenous protein binding 1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding tetrapyrrole binding heme binding electron transfer activity transition metal ion binding iron ion binding metal ion binding	response to stimulus response to chemical response to xenobiotic stimulus cellular response to stimulus regulation of biological process regulation of cellular process signaling biological regulation phospholipase C-activating serotonin receptor signaling pathway G protein-coupled serotonin receptor signaling pathway cell communication phospholipase C-activating G protein-coupled receptor signaling pathway G protein-coupled receptor signaling pathway cellular process response to stimulus response to chemical response to xenobiotic stimulus cellular response to stimulus regulation of biological process regulation of cellular process signaling biological regulation phospholipase C-activating serotonin receptor signaling pathway G protein-coupled serotonin receptor signaling pathway cell communication phospholipase C-activating G protein-coupled receptor signaling pathway G protein-coupled receptor signaling pathway cellular process signal transduction trans-synaptic signaling regulation of signaling modulation of chemical synaptic transmission cell-cell signaling presynaptic modulation of chemical synaptic transmission chemical synaptic transmission synaptic signaling regulation of trans-synaptic signaling anterograde trans-synaptic signaling regulation of cell communication regulation of defense response regulation of response to external stimulus defense response positive regulation of biological process response to external stimulus regulation of inflammatory response positive regulation of response to stimulus positive regulation of response to external stimulus positive regulation of inflammatory response regulation of response to stimulus regulation of response to stress response to stress positive regulation of defense response inflammatory response regulation of tube diameter multicellular organismal process system process regulation of tube size regulation of system process positive regulation of vasoconstriction circulatory system process regulation of blood circulation vascular process in circulatory system regulation of vasoconstriction positive regulation of multicellular organismal process regulation of multicellular organismal process blood vessel diameter maintenance regulation of biological quality vasoconstriction blood circulation regulation of anatomical structure size protein localization localization cellular localization protein localization to cytoskeleton protein localization to organelle cellular macromolecule localization macromolecule localization regulation of lipid metabolic process glycerophospholipid metabolic process lipid biosynthetic process positive regulation of phosphate metabolic process regulation of primary metabolic process phospholipid metabolic process positive regulation of metabolic process positive regulation of biosynthetic process regulation of phosphate metabolic process phosphate-containing compound metabolic process positive regulation of lipid metabolic process positive regulation of phosphatidylinositol biosynthetic process phosphorus metabolic process positive regulation of cellular process regulation of phosphatidylinositol biosynthetic process regulation of biosynthetic process phosphatidylinositol metabolic process positive regulation of phosphorus metabolic process glycerophospholipid biosynthetic process positive regulation of phospholipid biosynthetic process regulation of phospholipid metabolic process primary metabolic process phospholipid biosynthetic process regulation of phospholipid biosynthetic process phosphatidylinositol biosynthetic process positive regulation of phospholipid metabolic process biosynthetic process positive regulation of lipid biosynthetic process glycerolipid biosynthetic process organophosphate metabolic process organophosphate biosynthetic process metabolic process regulation of phosphorus metabolic process glycerolipid metabolic process regulation of lipid biosynthetic process regulation of metabolic process lipid metabolic process neuron apoptotic process positive regulation of programmed cell death regulation of apoptotic process regulation of programmed cell death cell death positive regulation of apoptotic process apoptotic process positive regulation of neuron apoptotic process programmed cell death regulation of neuron apoptotic process behavior learning or memory nervous system process cognition memory inorganic ion homeostasis intracellular calcium ion homeostasis homeostatic process calcium ion homeostasis cellular homeostasis chemical homeostasis intracellular monoatomic cation homeostasis monoatomic ion homeostasis intracellular chemical homeostasis monoatomic cation homeostasis intracellular monoatomic ion homeostasis regulation of execution phase of apoptosis positive regulation of execution phase of apoptosis execution phase of apoptosis regulation of body fluid levels homotypic cell-cell adhesion regulation of cell activation positive regulation of cell-cell adhesion cell adhesion cell-cell adhesion coagulation regulation of cell-cell adhesion response to wounding wound healing regulation of homotypic cell-cell adhesion positive regulation of cell adhesion regulation of cell adhesion cell activation hemostasis platelet aggregation blood coagulation regulation of platelet activation regulation of platelet aggregation positive regulation of homotypic cell-cell adhesion positive regulation of platelet aggregation platelet activation ribonucleotide catabolic process pyridine nucleotide catabolic process oxoacid metabolic process carbohydrate catabolic process carbohydrate derivative metabolic process organophosphate catabolic process nucleoside phosphate catabolic process organic acid metabolic process nucleobase-containing compound metabolic process glycolytic process pyridine-containing compound metabolic process small molecule metabolic process purine ribonucleotide catabolic process pyridine nucleotide metabolic process nucleoside phosphate metabolic process nicotinamide nucleotide metabolic process pyruvate metabolic process purine nucleoside diphosphate metabolic process purine-containing compound catabolic process nucleotide metabolic process nucleobase-containing compound catabolic process nucleoside diphosphate metabolic process purine nucleoside diphosphate catabolic process nucleoside diphosphate catabolic process nucleoside triphosphate metabolic process monocarboxylic acid metabolic process purine ribonucleotide metabolic process pyridine-containing compound catabolic process ribose phosphate metabolic process catabolic process ATP metabolic process purine nucleotide metabolic process ribonucleotide metabolic process nucleobase-containing small molecule metabolic process purine ribonucleoside triphosphate metabolic process ribonucleoside diphosphate metabolic process ribonucleoside diphosphate catabolic process nucleotide catabolic process ribonucleoside triphosphate metabolic process purine nucleoside triphosphate metabolic process purine nucleotide catabolic process carbohydrate metabolic process carbohydrate derivative catabolic process ADP catabolic process carboxylic acid metabolic process generation of precursor metabolites and energy purine-containing compound metabolic process ADP metabolic process purine ribonucleoside diphosphate metabolic process purine ribonucleoside diphosphate catabolic process detection of external stimulus detection of stimulus involved in sensory perception of pain sensory perception of temperature stimulus sensory perception of pain detection of temperature stimulus involved in sensory perception response to temperature stimulus detection of abiotic stimulus detection of stimulus sensory perception detection of temperature stimulus response to abiotic stimulus detection of stimulus involved in sensory perception detection of temperature stimulus involved in sensory perception of pain negative regulation of signaling synaptic transmission, glutamatergic negative regulation of biological process regulation of synaptic transmission, glutamatergic negative regulation of synaptic transmission negative regulation of cell communication negative regulation of cellular process negative regulation of synaptic transmission, glutamatergic smooth muscle contraction urinary bladder smooth muscle contraction urinary tract smooth muscle contraction muscle contraction muscle system process developmental process fat cell differentiation positive regulation of fat cell differentiation regulation of developmental process cellular developmental process regulation of cell differentiation positive regulation of developmental process positive regulation of cell differentiation cell differentiation regulation of fat cell differentiation G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger negative regulation of potassium ion transport regulation of localization regulation of potassium ion transport transport regulation of transport negative regulation of monoatomic ion transport regulation of monoatomic ion transport negative regulation of transport establishment of localization metal ion transport monoatomic ion transport potassium ion transport monoatomic cation transport regulation of metal ion transport positive regulation of cytosolic calcium ion concentration regulation of heat generation positive regulation of heat generation heat generation multicellular organismal-level homeostasis temperature homeostasis regulation of generation of precursor metabolites and energy regulation of ATP metabolic process regulation of purine nucleotide catabolic process positive regulation of nucleotide catabolic process regulation of small molecule metabolic process regulation of nucleotide metabolic process regulation of nucleobase-containing compound metabolic process regulation of carbohydrate catabolic process positive regulation of nucleobase-containing compound metabolic process regulation of purine nucleotide metabolic process positive regulation of ATP metabolic process regulation of nucleotide catabolic process positive regulation of carbohydrate metabolic process positive regulation of nucleotide metabolic process positive regulation of purine nucleotide catabolic process regulation of carbohydrate metabolic process positive regulation of glycolytic process regulation of catabolic process regulation of glycolytic process positive regulation of purine nucleotide metabolic process positive regulation of catabolic process positive regulation of small molecule metabolic process adult behavior response to oxygen-containing compound response to nitrogen compound response to alkaloid behavioral response to cocaine response to organic cyclic compound response to cocaine detection of mechanical stimulus involved in sensory perception of pain response to mechanical stimulus detection of mechanical stimulus involved in sensory perception sensory perception of mechanical stimulus detection of mechanical stimulus positive regulation of cell communication positive regulation of signal transduction regulation of signal transduction intracellular signal transduction positive regulation of ERK1 and ERK2 cascade regulation of intracellular signal transduction intracellular signaling cassette positive regulation of MAPK cascade positive regulation of intracellular signal transduction regulation of MAPK cascade MAPK cascade ERK1 and ERK2 cascade regulation of ERK1 and ERK2 cascade positive regulation of signaling phosphatidylinositol 3-kinase/protein kinase B signal transduction learning nonassociative learning sensitization monoamine transport nitrogen compound transport regulation of catecholamine secretion organic hydroxy compound transport dopamine transport secretion by cell regulation of secretion by cell catecholamine transport signal release secretion export from cell dopamine secretion regulation of secretion catecholamine secretion amine transport regulation of amine transport regulation of dopamine secretion cellular response to nitrogen compound response to dopamine cellular response to dopamine response to monoamine response to catecholamine cellular response to catecholamine stimulus serotonin receptor signaling pathway cellular response to organic cyclic compound cellular response to oxygen-containing compound cellular response to chemical stimulus cellular response to monoamine stimulus cell population proliferation positive regulation of cell population proliferation regulation of cell population proliferation monoatomic ion transmembrane transport negative regulation of sequestering of calcium ion calcium ion transport maintenance of location in cell monoatomic cation transmembrane transport regulation of sequestering of calcium ion calcium ion transmembrane import into cytosol sequestering of calcium ion inorganic ion transmembrane transport inorganic cation transmembrane transport maintenance of location transmembrane transport release of sequestered calcium ion into cytosol calcium ion transmembrane transport vascular associated smooth muscle contraction artery smooth muscle contraction tonic smooth muscle contraction regulation of DNA biosynthetic process positive regulation of macromolecule biosynthetic process nucleic acid biosynthetic process positive regulation of macromolecule metabolic process positive regulation of DNA biosynthetic process regulation of macromolecule metabolic process DNA metabolic process nucleobase-containing compound biosynthetic process macromolecule biosynthetic process nucleic acid metabolic process positive regulation of DNA metabolic process regulation of macromolecule biosynthetic process macromolecule metabolic process DNA biosynthetic process regulation of DNA metabolic process regulation of immune effector process cytokine production regulation of cytokine production positive regulation of immune effector process regulation of immune system process cytokine production involved in immune response positive regulation of immune system process production of molecular mediator of immune response regulation of cytokine production involved in immune response immune response gene expression immune effector process regulation of gene expression positive regulation of gene expression immune system process positive regulation of cytokine production involved in immune response positive regulation of production of molecular mediator of immune response regulation of production of molecular mediator of immune response positive regulation of cytokine production regulation of protein modification process positive regulation of phosphorylation regulation of protein phosphorylation positive regulation of protein metabolic process peptidyl-tyrosine modification positive regulation of peptidyl-tyrosine phosphorylation positive regulation of protein modification process peptidyl-amino acid modification protein metabolic process protein modification process positive regulation of protein phosphorylation protein phosphorylation phosphorylation regulation of protein metabolic process regulation of peptidyl-tyrosine phosphorylation macromolecule modification regulation of phosphorylation peptidyl-tyrosine phosphorylation electron transport chain	cell periphery postsynapse cellular anatomical structure postsynaptic membrane synapse cell junction membrane plasma membrane plasma membrane region synaptic membrane protein-containing complex G protein-coupled serotonin receptor complex receptor complex presynapse cell periphery postsynapse cellular anatomical structure postsynaptic membrane synapse cell junction membrane plasma membrane plasma membrane region synaptic membrane protein-containing complex G protein-coupled serotonin receptor complex receptor complex presynapse presynaptic membrane somatodendritic compartment cell projection dendrite dendritic tree neuron projection plasma membrane bounded cell projection glutamatergic synapse dendritic shaft cell body neuronal cell body axon membrane microdomain membrane raft plasma membrane raft caveola cell body fiber membrane-bounded organelle intracellular organelle intracellular anatomical structure cytoplasmic vesicle organelle intracellular vesicle cytoplasm intracellular membrane-bounded organelle vesicle polymeric cytoskeletal fiber neurofilament intracellular membraneless organelle intermediate filament cytoskeleton cytoskeleton membraneless organelle intermediate filament supramolecular fiber supramolecular polymer supramolecular complex periplasmic space

InterPro: Protein Family Classification InterPro Database Homepage

Chains	Accession	Name	Type
A, B, C	IPR002231	5-hydroxytryptamine receptor family	Family
A, B, C	IPR000276	G protein-coupled receptor, rhodopsin-like	Family
A, B, C	IPR017452	GPCR, rhodopsin-like, 7TM	Domain
A, B, C	IPR000455	5-Hydroxytryptamine 2A receptor	Family
A, B, C	IPR010980	Cytochrome c/b562	Homologous Superfamily
A, B, C	IPR009155	Cytochrome b562	Family

Pharos: Disease Associations Pharos Homepage Annotation

Chains	Drug Target	Associated Disease
A, B, C	Pharos: P28223	schizophrenia obsessive-compulsive disorder bipolar disorder schizoaffective disorder major depressive disorder alcohol abuse obesity disorder lingual-facial-buccal dyskinesia cocaine dependence Fever anorexia nervosa autism basal ganglia disease seasonal affective disorder metabolic disease schizophrenia obsessive-compulsive disorder bipolar disorder schizoaffective disorder major depressive disorder alcohol abuse obesity disorder lingual-facial-buccal dyskinesia cocaine dependence Fever anorexia nervosa autism basal ganglia disease seasonal affective disorder metabolic disease Parkinson disease cocaine abuse interstitial cystitis pilocytic astrocytoma primitive neuroectodermal tumor psychotic disorder malignant ependymoma alcohol dependence allergic rhinitis glioblastoma astrocytic tumor ovarian cancer large cell medulloblastoma malignant glioma depressive disorder fibromyalgia anxiety disorder atopic conjunctivitis urticaria hypoactive sexual desire disorder oligodendroglioma chronic obstructive pulmonary disease acute intermittent porphyria pulmonary arterial hypertension schizophreniform disorder medulloblastoma familial dermatographia migraine disorder angioedema mood disorder atypical teratoid rhabdoid tumor

Membrane Protein Annotation: OPM OPM Database Homepage

Chains	External Link	Type	Class	Superfamily	Family
A, B, C	OPM	Transmembrane	Alpha-helical polytopic	Rhodopsin-like receptors and pumps	G-protein coupled receptors, family A

Membrane Protein Annotation: PDBTM PDBTM Database Homepage

Chains	External Link	Comment
A, B, C	PDBTM	Annotated as membrane protein by PDBTM

Membrane Protein Annotation: MemProtMD MemProtMD Database Homepage

Chains	External Link	Comment
A, B, C	MemProtMD	Annotated as membrane protein by MemProtMD

Membrane Protein Annotation: mpstruc mpstruc Database Homepage

Chains	Resource Link	Group	Subgroup	Protein
A, B, C	mpstruc	TRANSMEMBRANE PROTEINS: ALPHA-HELICAL	G Protein-Coupled Receptors: Class A	5-HT_2A serotonin receptor complexed with G_��q and hallucinogen

RCSB PDB Core Operations are funded by the U.S. National Science Foundation (DBI-2321666), the US Department of Energy (DE-SC0019749), and the National Cancer Institute, National Institute of Allergy and Infectious Diseases, and National Institute of General Medical Sciences of the National Institutes of Health under grant R01GM157729.