CGP 20712A [Ligand Id: 541] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL280822 (CGP-20712A)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
  • 8.1
1 CHEMBL280822_lig_chart_1 Beta-1 adrenergic receptor HumanMouseRat
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • This target only has 1 pki data point
  • 6
2 CHEMBL280822_lig_chart_2 Beta-2 adrenergic receptor Human
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
  • This target only has 1 pki data point
  • 5.7
3 CHEMBL280822_lig_chart_3 Beta-3 adrenergic receptor Human
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • This target only has 1 pki data point
  • 6.22
4 CHEMBL280822_lig_chart_4 Serotonin 1a (5-HT1a) receptor Rat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of CGP12177-induced [3H]cAMP accumulation F 7.22 pKd 60.26 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Displacement of [3H]-CGP12177 from human beta1 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis B 8.79 pKd 1.62 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Displacement of [3H](-)CGP12177 from human beta1-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method B 8.96 pKd 1.1 nM Kd ACS Med Chem Lett (2017) 8: 481-485 [PMID:28523097]
ChEMBL Antagonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 9.48 pKd 0.33 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Displacement of [3H]CGP12177 from human beta1 adrenoceptor expressed in HEK293T cell membranes B 8.92 pKi 1.2 nM Ki Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
GtoPdb - - 9.2 pKi 0.63 nM Ki Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020];
Br J Pharmacol (2005) 144: 317-22 [PMID:15655528];
J Pharmacol Exp Ther (1999) 290: 649-55 [PMID:10411574]
β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971]
ChEMBL Displacement of [3H]CGP12177 from mouse beta1 adrenoceptor expressed in HEK293T cell membranes B 8.85 pKi 1.4 nM Ki Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor Y356A mutant expressed in CHO cells F 5 pKi 10000 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor S190A mutant expressed in CHO cells F 6.1 pKi 794.33 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor W134A mutant expressed in CHO cells F 8.1 pKi 7.94 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat beta-1 adrenergic receptor Y356F mutant expressed in CHO cells F 8.7 pKi 2 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
ChEMBL Antagonist activity at rat wild type beta-1 adrenergic receptor expressed in CHO cells F 8.9 pKi 1.26 nM Ki J. Med. Chem. (2006) 49: 3467-3477 [PMID:16759089]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [3H]-CGP12177 from human beta2 adrenoceptor expressed in CHOK1 cells after 2 hrs by scintillation counting analysis B 5.82 pKd 1513.56 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Displacement of [3H](-)CGP12177 from human beta2-AR expressed in CHOK1 cells after 2 hrs by TopCount microscintillation counting method B 5.84 pKd 1445.44 nM Kd ACS Med Chem Lett (2017) 8: 481-485 [PMID:28523097]
ChEMBL Antagonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 5.98 pKd 1047.13 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
ChEMBL Displacement of [3H]CGP12177 from human beta2 adrenoceptor expressed in CHO cell membranes B 6 pKi 1000 nM Ki Bioorg Med Chem (2019) 27: 2959-2971 [PMID:31151791]
ChEMBL Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs F 5 pEC50 10000 nM EC50 J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL Antagonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as inhibition of cimaterol-induced [3H]cAMP accumulation incubated for 15 mins prior to cimaterol induction measured after 5 hrs F 5.26 pKd 5495.41 nM Kd J. Med. Chem. (2013) 56: 3852-3865 [PMID:23614528]
GtoPdb - - 5.7 pKi - - - Eur J Pharmacol (1999) 367: 431-5 [PMID:10079020];
Br J Pharmacol (2005) 144: 317-22 [PMID:15655528];
J Pharmacol Exp Ther (1999) 290: 649-55 [PMID:10411574];
Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement B 6.22 pKi 602.56 nM Ki J. Med. Chem. (1996) 39: 126-134 [PMID:8568799]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]