ChEMBL ligand: CHEMBL500 (Apo-pindol, Betadren, Betapindol, Blocklin-l, Calvisken, Carvisken, Decreten, Dl-lb-46, Dl-pindolol, Durapindol, Glauco-visken, LB-46, NSC-757276, Pectobloc, Pinbetol, Pindolol, Prinodolol, Pynastin, (rs)-pindolol, Visken)
β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] 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 Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] 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!
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] There should be some charts here, you may need to enable JavaScript!
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] There should be some charts here, you may need to enable JavaScript!
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] 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 beta-1 adrenergic receptor site 1 expressed in CGP 12177-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	F	5	pKd	<10000	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Displacement of [3H]-CGP 12177 from human beta-1 adrenergic receptor expressed in CHOK1 cells	B	8.58	pKd	2.63	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Antagonist activity at human beta-1 adrenergic receptor site 1 expressed in cimeterol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	F	8.62	pKd	2.4	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)	B	9.27	pKi	0.53	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity at human adrenergic beta-1 receptor	B	9.28	pKi	0.52	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5600-5604 [PMID:17804228]
GtoPdb	-	-	9.3	pKi	-	-	-	Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Bioorg Med Chem Lett (2007) 17: 5600-4 [PMID:17804228]
GtoPdb	-	-	9.7	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 525-32 [PMID:15060759]; Mol Pharmacol (2003) 64: 1357-69 [PMID:14645666]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]
ChEMBL	DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol)	B	9.04	pIC50	0.92	nM	IC50	DrugMatrix in vitro pharmacology data
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL	Antagonist activity at human beta-2 adrenergic receptor expressed in salbutamol-stimulated CHO-K1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	F	9.18	pKd	0.66	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Displacement of [3H]-CGP 12177 from human beta-2 adrenergic receptor expressed in CHOK1 cells	B	9.27	pKd	0.54	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Binding affinity at human adrenergic beta2 receptor	B	9.4	pKi	0.4	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5600-5604 [PMID:17804228]
GtoPdb	-	-	9.4	pKi	-	-	-	Bioorg Med Chem Lett (2007) 17: 5600-4 [PMID:17804228]
GtoPdb	-	-	9.4	pKi	0.4	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5600-4 [PMID:17804228]
ChEMBL	DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)	B	9.42	pKi	0.38	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)	B	9.26	pIC50	0.55	nM	IC50	DrugMatrix in vitro pharmacology data
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL	Antagonist activity at human beta-3 adrenergic receptor expressed in fenoterol-stimulated CHOK1 cells assessed as CRE-SPAP level by fluorescence correlation spectroscopic analysis	F	6	pKd	<1000	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
ChEMBL	Displacement of [3H]-CGP 12177 from human beta-3 adrenergic receptor expressed in CHOK1 cells	B	6.78	pKd	165.96	nM	Kd	J Med Chem (2011) 54: 6874-6887 [PMID:21870877]
GtoPdb	-	-	7.1	pKi	-	-	-	Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]
ChEMBL	DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)	B	7.18	pKi	66	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)	B	7.06	pIC50	88	nM	IC50	DrugMatrix in vitro pharmacology data
GtoPdb	-	-	7.4	pEC50	-	-	-	Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Binding affinity to 5HT1A receptor	B	7.2	pKd	63.1	nM	Kd	J Med Chem (2009) 52: 6107-6125 [PMID:19754201]
ChEMBL	Inhibition constant against 5-hydroxytryptamine 1A receptor	B	6.96	pKi	110	nM	Ki	J Med Chem (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL	Antagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as inhibition of 5-HT-stimulated [35S]GTP-gamma-S binding	F	7.09	pKi	81.1	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5600-5604 [PMID:17804228]
ChEMBL	Displacement of specific [3H]- 5-HT binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells	B	7.62	pKi	24	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3243-3248 [PMID:10576696]
ChEMBL	Displacement of [3H]DPAT from human 5HT1A receptor	B	7.65	pKi	22.4	nM	Ki	Bioorg Med Chem Lett (2007) 17: 5600-5604 [PMID:17804228]
GtoPdb	-	-	8.1	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 205-17 [PMID:9550290]
ChEMBL	Stimulation of [35S]- GIPyS binding to cloned human 5-hydroxytryptamine 1A receptor stably expressed in HeLa cells	B	7.57	pEC50	27	nM	EC50	Bioorg Med Chem Lett (1999) 9: 3243-3248 [PMID:10576696]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)	B	7.57	pKi	27	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement	B	7.66	pKi	21.88	nM	Ki	J Med Chem (1996) 39: 126-134 [PMID:8568799]
ChEMBL	Evaluated for the binding affinity to hippocampus striatal membranes at 5-hydroxytryptamine 1A receptor binding site by using [3H]-8-OH- DPAT as a radioligand.	B	7.7	pKi	20	nM	Ki	J Med Chem (1987) 30: 1-12 [PMID:3543362]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)	B	7.32	pIC50	48	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL	Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptor	F	5	pKi	>10000	nM	Ki	J Med Chem (1997) 40: 4415-4419 [PMID:9435911]
ChEMBL	Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptor	F	5.59	pKi	2600	nM	Ki	J Med Chem (1997) 40: 4415-4419 [PMID:9435911]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL	Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.	B	7.1	pKi	80	nM	Ki	J Med Chem (1987) 30: 1-12 [PMID:3543362]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL	Evaluated for the binding affinity to porcine choroid plexus at 5-hydroxytryptamine 2C receptor binding site by using [3H]-MES as a radioligand.	B	4.27	pKi	54000	nM	Ki	J Med Chem (1987) 30: 1-12 [PMID:3543362]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Displacement of specific [3H]- citalopram binding to 5-HT uptake site in rat whole cortex	B	5.15	pKi	>7000	nM	Ki	Bioorg Med Chem Lett (1999) 9: 3243-3248 [PMID:10576696]
5-HT2A receptor in Human [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb	-	-	5	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
GtoPdb	-	-	5	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb	-	-	5.7	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
GtoPdb	-	-	5.7	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]

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]