cabergoline [Ligand Id: 37] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1201087 (Cabaser, Cabergolina, Cabergoline, Dostinex, FCE 21336, FCE-21336, Velactis)
  • 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • D1 receptor/D(1A) dopamine receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
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  • α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
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  • α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
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  • D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
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  • D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [125I](+/-)DOI from human 5-HT2B receptor transfected in CHO cell membrane after 60 mins by scintillation counting analysis B 8.85 pKi 1.4 nM Ki ACS Med Chem Lett (2013) 4: 254-258 [PMID:23606928]
GtoPdb - - 8.9 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
GtoPdb - - 7.9 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL GPCR PRESTO-Tango dose-response in agonist mode with target: ADRA2A F 6.54 pEC50 285.43 nM EC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
D1 receptor/D(1A) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Binding affinity to D1 receptor (unknown origin) assessed as inhibition constant B 5.42 pKi 3800 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
GtoPdb - - 6.7 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL Binding affinity to dopamine D1 receptor (unknown origin) assessed as inhibition constant B 8.85 pKi 1.4 nM Ki RSC Med Chem (2024) 15: 788-808 [PMID:38516587]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
GtoPdb - - 9.2 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
ChEMBL Binding affinity to D2 receptor (unknown origin) assessed as inhibition constant B 9.44 pKi 0.36 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
ChEMBL Binding affinity to D2L receptor (unknown origin) assessed as inhibition constant B 9.44 pKi 0.36 nM Ki J Med Chem (2024) 67: 12463-12484 [PMID:39038276]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 7.7 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT1B receptor in Human [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT1D receptor in Human [GtoPdb: 3] [UniProtKB: P28221]
GtoPdb - - 8.1 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 8.2 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 6.2 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
α1A-adrenoceptor in Human [GtoPdb: 22] [UniProtKB: P35348]
GtoPdb - - 6.5 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
α2B-adrenoceptor in Human [GtoPdb: 26] [UniProtKB: P18089]
GtoPdb - - 7.1 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
α2C-adrenoceptor in Human [GtoPdb: 27] [UniProtKB: P18825]
GtoPdb - - 7.7 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
D3 receptor in Human [GtoPdb: 216] [UniProtKB: P35462]
GtoPdb - - 9.1 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
D4 receptor in Human [GtoPdb: 217] [UniProtKB: P21917]
GtoPdb - - 7.3 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]
D5 receptor in Human [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 7.7 pKi - - - J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]