ChEMBL ligand: CHEMBL31354 (WAY-100635)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] There should be some charts here, you may need to enable JavaScript!
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] There should be some charts here, you may need to enable JavaScript!
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] There should be some charts here, you may need to enable JavaScript!
D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] 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] There should be some charts here, you may need to enable JavaScript!
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Mouse [ChEMBL: CHEMBL4297] [GtoPdb: 3] [UniProtKB: Q61224] There should be some charts here, you may need to enable JavaScript!
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] SERT/Serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] 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
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
ChEMBL	Inhibition of adrenergic alpha1A receptor	B	7.7	pKi	20	nM	Ki	J Med Chem (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL	Displacement [3H]prazosin of human recombinant alpha1A adrenergic receptor expressed in CHO cells by rapid filtration technique	B	7.73	pKi	18.62	nM	Ki	Eur J Med Chem (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL	Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1A expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting	B	7.73	pKi	18.62	nM	Ki	Eur J Med Chem (2019) 176: 310-325 [PMID:31112892]
ChEMBL	Displacement of [3H]Prazosin from human recombinant alpha 1A adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay	B	7.73	pKi	18.62	nM	Ki	Eur J Med Chem (2019) 168: 461-473 [PMID:30844609]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL	Inhibition of adrenergic Alpha-1B receptor	B	6.49	pKi	322	nM	Ki	J Med Chem (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL	Displacement [3H]prazosin of human recombinant Alpha-1B adrenergic receptor expressed in CHO cells by rapid filtration technique	B	7.18	pKi	66.07	nM	Ki	Eur J Med Chem (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL	Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1B expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter	B	7.18	pKi	66.07	nM	Ki	Eur J Med Chem (2019) 176: 310-325 [PMID:31112892]
ChEMBL	Displacement of [3H]Prazosin from human recombinant alpha 1B adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay	B	7.18	pKi	66.07	nM	Ki	Eur J Med Chem (2019) 168: 461-473 [PMID:30844609]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL	Displacement [3H]prazosin of human recombinant Alpha-1D adrenergic receptor expressed in CHO cells by rapid filtration technique	B	8.34	pKi	4.57	nM	Ki	Eur J Med Chem (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL	Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1D expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter	B	8.34	pKi	4.57	nM	Ki	Eur J Med Chem (2019) 176: 310-325 [PMID:31112892]
ChEMBL	Displacement of [3H]Prazosin from human recombinant alpha 1D adrenergic receptor expressed in CHO cells incubated for 30 mins by radioligand competition binding assay	B	8.34	pKi	4.57	nM	Ki	Eur J Med Chem (2019) 168: 461-473 [PMID:30844609]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Inhibition of dopamine D4 receptor	B	7.8	pKi	16	nM	Ki	J Med Chem (2011) 54: 3480-3491 [PMID:21520940]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb	-	-	9.5	pKd	0.3	nM	Kd	Life Sci (1997) 60: 653-65 [PMID:9048968]
ChEMBL	Inhibition of 5HT1A receptor	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL	Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells after 120 mins	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2009) 52: 7892-7896 [PMID:19705871]
ChEMBL	Binding affinity against human 5-hydroxytryptamine 1A receptor in CHO cells labeled with [3H]8-OH-DPAT radioligand	B	9.02	pKi	0.96	nM	Ki	J Med Chem (2004) 47: 3823-3842 [PMID:15239661]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells	B	9.05	pKi	0.9	nM	Ki	J Med Chem (2010) 53: 4066-4084 [PMID:20443629]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells	B	9.05	pKi	0.9	nM	Ki	Bioorg Med Chem (2008) 16: 6707-6723 [PMID:18571421]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5HT1A receptor expressed in CHO cells	B	9.05	pKi	0.9	nM	Ki	J Med Chem (2009) 52: 4955-4959 [PMID:19719241]
ChEMBL	Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor	B	9.1	pKi	0.79	nM	Ki	J Med Chem (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL	In vitro inhibition of [3H]- 8-OH-DPAT binding to cloned cell line containing human 5-hydroxytryptamine 1A receptor	B	9.23	pKi	0.59	nM	Ki	J Med Chem (1999) 42: 1576-1586 [PMID:10229627]
ChEMBL	Binding affinity at human 5-hydroxytryptamine 1A receptor by inhibition of [3H]8-OH-DPAT binding in Chinese hamster ovary cell line	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2002) 45: 165-176 [PMID:11754589]
ChEMBL	Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting	B	9.41	pKi	0.39	nM	Ki	J Med Chem (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL	Displacement [3H]8-OH-DPAT of human cloned 5HT1A receptor expressed in human HeLa cells by rapid filtration technique	B	9.48	pKi	0.33	nM	Ki	Eur J Med Chem (2010) 45: 3740-3751 [PMID:20605276]
ChEMBL	Displacement of [3H]8-OH-DPAT from human cloned 5HT-1AR transfected in HeLa cells incubated for 30 mins by liquid scintillation counter	B	9.48	pKi	0.33	nM	Ki	Eur J Med Chem (2019) 176: 310-325 [PMID:31112892]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human recombinant 5-HT1A receptor expressed in human HeLa cells incubated for 30 mins by radioligand competition binding assay	B	9.48	pKi	0.33	nM	Ki	Eur J Med Chem (2019) 168: 461-473 [PMID:30844609]
ChEMBL	Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor	B	9.8	pKi	0.16	nM	Ki	J Med Chem (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL	Antagonist activity at serotonin 5-HT1A receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of serotonin-induced calcium flux after 15 mins by calcium 4-dye based FLIPR assay	F	7.95	pIC50	11.3	nM	IC50	J Med Chem (2018) 61: 10017-10039 [PMID:30383372]
ChEMBL	Antagonist activity at human 5HT1A receptor expressed in CHO cells assessed as blockade of 8-OH-DPAT-induced inhibition of forskolin-stimulated increase in cAMP level	F	8.15	pIC50	7.1	nM	IC50	J Med Chem (2010) 53: 4066-4084 [PMID:20443629]
ChEMBL	Antagonist activity at human 5HT1A receptor expressed in CHO-K1 cells assessed as inhibition of 5HT-induced calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation at room temperature and subsequent 5HT addition by calcium 4 dye based FLIPR assay	F	8.55	pIC50	2.8	nM	IC50	Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805]
ChEMBL	Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor expressed in HEK293 EBNA cells after 1 hr by liquid scintillation counting	B	9.04	pIC50	0.91	nM	IC50	J Med Chem (2011) 54: 3480-3491 [PMID:21520940]
ChEMBL	Effective concentration against binding of radioligand [35S]GTP-gamma-S in CHO cells expressing human 5-hydroxytryptamine 1A receptor	F	8.15	pEC50	7.1	nM	EC50	J Med Chem (2004) 47: 3823-3842 [PMID:15239661]
ChEMBL	Effective concentration against human 5-hydroxytryptamine 1A receptor using cAMP as radioligand in CHO cells	B	8.15	pEC50	7.1	nM	EC50	J Med Chem (2004) 47: 3823-3842 [PMID:15239661]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Compound was tested for its potency against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.	F	9.69	pKd	0.2	nM	Kd	Bioorg Med Chem Lett (1998) 8: 2457-2462 [PMID:9873561]
ChEMBL	In vitro binding affinity for 5-hydroxytryptamine 1A receptor was determined by measuring specific inhibition of [125I]-binding to rat hippocampal membrane preparations	B	10	pKd	0.1	nM	Kd	J Med Chem (1998) 41: 157-166 [PMID:9457239]
ChEMBL	Inhibition of binding of [125I]8-OH-PIPAT ligand to 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates	B	9.08	pKi	0.84	nM	Ki	J Med Chem (1994) 37: 1406-1407 [PMID:8182697]
ChEMBL	Compound was tested for inhibition constant against 5-hydroxytryptamine 1A receptor in rat frontal cortex membranes.	B	9.3	pKi	0.5	nM	Ki	Bioorg Med Chem Lett (1998) 8: 2457-2462 [PMID:9873561]
ChEMBL	In vitro binding affinity to 5-hydroxytryptamine 1A receptor using [125I](R)-(+)-trans-8-OH-PIPAT as radioligand in rat hippocampal homogenate	B	8.66	pIC50	2.2	nM	IC50	J Med Chem (1994) 37: 4572-4575 [PMID:7799409]
ChEMBL	Inhibitory activity against 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates	B	8.66	pIC50	2.2	nM	IC50	J Med Chem (1994) 37: 1406-1407 [PMID:8182697]
ChEMBL	In vitro affinity against 5-hydroxytryptamine 1A receptor using [3H]-8-OH-DPAT in rat hippocampus	B	9.43	pIC50	0.37	nM	IC50	J Med Chem (2000) 43: 432-439 [PMID:10669570]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL	Inhibition of 5HT1B receptor	B	7.62	pKi	24	nM	Ki	J Med Chem (2011) 54: 3480-3491 [PMID:21520940]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4297] [GtoPdb: 3] [UniProtKB: Q61224]
ChEMBL	Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 1)	F	8.96	pKi	1.09	nM	Ki	J Med Chem (1999) 42: 1576-1586 [PMID:10229627]
ChEMBL	Receptor-linked G protein activation at 5-hydroxytryptamine receptor was determined by measuring the stimulation of [35S]GTP-gamma-S, binding (Experiment 2)	F	9.47	pKi	0.34	nM	Ki	J Med Chem (1999) 42: 1576-1586 [PMID:10229627]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL	Inhibition of 5HT7 receptor	B	5	pKi	10000	nM	Ki	J Med Chem (2011) 54: 3480-3491 [PMID:21520940]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	Inhibition concentration against [3H]5-HT uptake by human serotonin transporter in JAR cells	B	5.35	pIC50	>4500	nM	IC50	J Med Chem (2004) 47: 3823-3842 [PMID:15239661]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL	Binding affinity against serotonin transporter in rat cortical tissues using radioligand [3H]paroxetine	B	6	pKi	>1000	nM	Ki	J Med Chem (2004) 47: 3823-3842 [PMID:15239661]

ChEMBL data shown on this page come from version 32:

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]