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5A8E

thermostabilised beta1-adrenoceptor with rationally designed inverse agonist 7-methylcyanopindolol bound

Functional Information from GO Data
ChainGOidnamespacecontents
A0004930molecular_functionG protein-coupled receptor activity
A0004935molecular_functionadrenergic receptor activity
A0004940molecular_functionbeta1-adrenergic receptor activity
A0007186biological_processG protein-coupled receptor signaling pathway
A0007189biological_processadenylate cyclase-activating G protein-coupled receptor signaling pathway
A0016020cellular_componentmembrane
A0045823biological_processpositive regulation of heart contraction
Functional Information from PDB Data
site_idAC1
Number of Residues6
DetailsBINDING SITE FOR RESIDUE NA A 401
ChainResidue
ACYS192
AASP195
ACYS198
AHOH3009
AHOH3014
AHOH3015

site_idAC2
Number of Residues5
DetailsBINDING SITE FOR RESIDUE NA A 402
ChainResidue
AHOH3004
AHOH3022
AASP87
ASER128
AHOH3003

site_idAC3
Number of Residues13
DetailsBINDING SITE FOR RESIDUE XTK A 501
ChainResidue
ATRP117
AASP121
AVAL122
ATHR203
AALA208
ASER211
ASER215
ATRP303
APHE306
APHE307
AASN310
AASN329
ATYR333

site_idAC4
Number of Residues10
DetailsBINDING SITE FOR RESIDUE MHA A 801
ChainResidue
AGLY110
ASER111
APRO196
ALYS287
ALYS290
ATHR291
AARG345
ASER346
AHOH3008
AHOH3026

site_idAC5
Number of Residues7
DetailsBINDING SITE FOR RESIDUE OLC A 2001
ChainResidue
AALA227
AILE238
AARG239
AHIS286
ALEU289
AGLY293
AOLC2002

site_idAC6
Number of Residues8
DetailsBINDING SITE FOR RESIDUE OLC A 2002
ChainResidue
ATRP107
ALEU108
AASP195
AGLY197
ALYS287
ALYS290
AGLY293
AOLC2001

site_idAC7
Number of Residues2
DetailsBINDING SITE FOR RESIDUE OLC A 2003
ChainResidue
ATYR140
ATYR140

site_idAC8
Number of Residues9
DetailsBINDING SITE FOR RESIDUE OLC A 2004
ChainResidue
AGLN73
ATHR74
ALEU75
ATHR76
AARG139
AILE143
AARG155
AGLU285
AALA288

site_idAC9
Number of Residues6
DetailsBINDING SITE FOR RESIDUE OLC A 2005
ChainResidue
ATRP181
AASP184
AASN204
AARG205
ALYS276
APHE315

Functional Information from PROSITE/UniProt
site_idPS00237
Number of Residues17
DetailsG_PROTEIN_RECEP_F1_1 G-protein coupled receptors family 1 signature. ASVwTLCVIAIDRYLaI
ChainResidueDetails
AALA127-ILE143

Functional Information from SwissProt/UniProt
site_idSWS_FT_FI1
Number of Residues28
DetailsTransmembrane: {"description":"Helical; Name=1"}
ChainResidueDetails

site_idSWS_FT_FI2
Number of Residues25
DetailsTopological domain: {"description":"Cytoplasmic","evidences":[{"source":"PubMed","id":"18594507","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI3
Number of Residues26
DetailsTransmembrane: {"description":"Helical; Name=2"}
ChainResidueDetails

site_idSWS_FT_FI4
Number of Residues40
DetailsTopological domain: {"description":"Extracellular","evidences":[{"source":"PubMed","id":"18594507","evidenceCode":"ECO:0000269"}]}
ChainResidueDetails

site_idSWS_FT_FI5
Number of Residues21
DetailsTransmembrane: {"description":"Helical; Name=3"}
ChainResidueDetails

site_idSWS_FT_FI6
Number of Residues23
DetailsTransmembrane: {"description":"Helical; Name=4"}
ChainResidueDetails

site_idSWS_FT_FI7
Number of Residues25
DetailsTransmembrane: {"description":"Helical; Name=5"}
ChainResidueDetails

site_idSWS_FT_FI8
Number of Residues29
DetailsTransmembrane: {"description":"Helical; Name=6"}
ChainResidueDetails

site_idSWS_FT_FI9
Number of Residues22
DetailsTransmembrane: {"description":"Helical; Name=7"}
ChainResidueDetails

site_idSWS_FT_FI10
Number of Residues3
DetailsBinding site: {"evidences":[{"source":"PubMed","id":"18594507","evidenceCode":"ECO:0000269"},{"source":"PDB","id":"2VT4","evidenceCode":"ECO:0007744"}]}
ChainResidueDetails

242842

PDB entries from 2025-10-08

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