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	Binding affinity to D4 receptor (unknown origin) assessed as dissociation constant	B	8.62	pKd	2.4	nM	Kd	J Med Chem (2022) 65: 10755-10808 [PMID:35939391]
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	Binding affinity to 5-HT1A receptor (unknown origin) assessed as dissociation constant	B	9.7	pKd	0.2	nM	Kd	J Med Chem (2022) 65: 10755-10808 [PMID:35939391]
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 5-HT1A receptor (unknown origin) by calcium flux assay	F	8.18	pIC50	6.6	nM	IC50	J Med Chem (2023) 66: 12141-12162 [PMID:37646374]
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	Displacement of [3H]-8-OH-DPAT from Sprague-Dawley rat hippocampal membrane 5HT1A receptor	B	8.38	pIC50	4.2	nM	IC50	J Med Chem (2022) 65: 10755-10808 [PMID:35939391]
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 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]