CGP 20712A [Ligand Id: 541] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL280822 (CGP-20712A) |
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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 | - | - | - |
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]; Pharmacol Res Perspect (2016) 4: e00250 [PMID:27588207]; Mol Pharmacol (2015) 88: 1024-34 [PMID:26385885] |
| 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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
