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] There should be some charts here, you may need to enable JavaScript!
β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] There should be some charts here, you may need to enable JavaScript!
β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] There should be some charts here, you may need to enable JavaScript!
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] There should be some charts here, you may need to enable JavaScript!

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-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as inhibition of fenoterol-induced CRE-SPAP production by measuring rightward shift of the fenoterol concentration response curve measured after 5 hrs incubation	F	8.99	pKd	1.02	nM	Kd	Eur J Med Chem (2023) 246: 114961-114961 [PMID:36495629]
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	Antagonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as inhibition of fenoterol-induced CRE-SPAP production by measuring rightward shift of the fenoterol concentration response curve measured after 5 hrs incubation	F	5.7	pKd	1995.26	nM	Kd	Eur J Med Chem (2023) 246: 114961-114961 [PMID:36495629]
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-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as inhibition of fenoterol-induced CRE-SPAP production by measuring rightward shift of the fenoterol concentration response curve measured after 5 hrs incubation	F	5.13	pKd	7413.1	nM	Kd	Eur J Med Chem (2023) 246: 114961-114961 [PMID:36495629]
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 34:

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]