ChEMBL ligand: CHEMBL8618 (NAN-190)
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!
D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] 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 Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] 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] 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] There should be some charts here, you may need to enable JavaScript!
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] 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	Binding constant measured against Alpha-1A adrenergic receptor in human prostate; ++:moderately active	B	8.7	pKi	2	nM	Ki	Bioorg Med Chem Lett (2005) 15: 657-664 [PMID:15664832]
ChEMBL	Displacement of [125]HEAT from human adrenergic alpha-1a receptor expressed in CHO cells	B	9.59	pKi	0.26	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1646-1650 [PMID:17254786]
GtoPdb	-	-	10.1	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL	Displacement of [125]HEAT from human adrenergic alpha-1b receptor expressed in CHO cells	B	9.02	pKi	0.96	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1646-1650 [PMID:17254786]
GtoPdb	-	-	9.2	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
GtoPdb	-	-	9.2	pKi	-	-	-	Jpn J Pharmacol (2001) 86: 189-95 [PMID:11459121]
ChEMBL	Displacement of [125]HEAT from human adrenergic alpha-1d receptor expressed in CHO cells	B	9.52	pKi	0.3	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1646-1650 [PMID:17254786]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL	Compound was evaluated for binding affinity against Dopamine receptor D2 using [3H]raclopride as a radioligand	B	7.19	pKi	64	nM	Ki	Bioorg Med Chem Lett (1996) 6: 689-694
ChEMBL	Binding affinity towards dopamine receptor D2 using [3H]-raclopride radioligand.	B	7.19	pKi	64	nM	Ki	J Med Chem (1996) 39: 4439-4450 [PMID:8893838]
ChEMBL	In vitro binding affinity towards Dopamine receptor D2 in rat striatum was determined using [3H]spiperone as radioligand	B	7.5	pKi	31.62	nM	Ki	J Med Chem (1995) 38: 4044-4055 [PMID:7562940]
ChEMBL	In vitro ability to inhibit binding of radioligand [3H]spiroperidol to dopamine D2 receptor in rat striatal membranes	B	8.02	pKi	9.55	nM	Ki	J Med Chem (1994) 37: 99-104 [PMID:8289207]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry	B	7.06	pKi	87	nM	Ki	Eur J Med Chem (2014) 85: 716-726 [PMID:25128671]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5-HT1A expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assay	B	8.35	pKi	4.49	nM	Ki	Eur J Med Chem (2020) 199: 112395-112395 [PMID:32442850]
ChEMBL	Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in HEK293 cells after 120 mins	B	9.22	pKi	0.6	nM	Ki	J Med Chem (2009) 52: 7892-7896 [PMID:19705871]
GtoPdb	-	-	9.4	pKi	-	-	-	Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
ChEMBL	Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells assessed as inhibition of serotonin-induced calcium mobilization preincubated for 25 mins followed by serotonin induction measured for 30 secs by aequorin-derived luminescence assay	F	8.3	pIC50	5	nM	IC50	Eur J Med Chem (2017) 137: 108-116 [PMID:28575721]
ChEMBL	Antagonist activity at human 5-HT1A receptor expressed in CHO-K1 cells co-expressing Galpha16 assessed as decrease in serotonin calcium mobilization preincubated for 25 mins followed by serotonin challenge measured for 30 secs by aequorin-derived luminescence assay	F	8.33	pIC50	4.73	nM	IC50	Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027]
ChEMBL	Antagonist activity at human recombinant 5-HT1A receptor expressed in CHOK1 cells incubated for 25 mins followed by addition of methiothepin by microbeta2 scintillation counter	B	8.95	pIC50	1.12	nM	IC50	Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
ChEMBL	Antagonist activity at human recombinant 5-HT1A receptor expressed in CHOK1 cells incubated for 25 mins followed by addition of methiothepin by microbeta2 scintillation counter	B	8.96	pIC50	1.1	nM	IC50	Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	In vitro ability to inhibit binding of radioligand [3H]8-OH-DPAT to 5-hydroxytryptamine 1A receptor in rat cerebral cortex	B	8.88	pKi	1.32	nM	Ki	J Med Chem (1994) 37: 99-104 [PMID:8289207]
ChEMBL	In vitro ability to displace [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor sites of rat brain cortex.	B	8.9	pKi	1.26	nM	Ki	J Med Chem (1995) 38: 1273-1277 [PMID:7731013]
ChEMBL	Binding affinity at 5-hydroxytryptamine 1A receptor	B	9.15	pKi	0.71	nM	Ki	J Med Chem (1995) 38: 4044-4055 [PMID:7562940]
ChEMBL	Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1996) 39: 126-134 [PMID:8568799]
ChEMBL	In vitro binding affinity for 5-hydroxytryptamine 1A receptor in rat hippocampal membranes by [125I]-labeled agonist displacement.	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1998) 41: 157-166 [PMID:9457239]
ChEMBL	In vitro binding affinity to 5-hydroxytryptamine 1A receptor using [125I](R)-(+)-trans-8-OH-PIPAT as radioligand in rat hippocampal homogenate	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1994) 37: 4572-4575 [PMID:7799409]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1A receptor using 0.1 nM [3H]-8-OH-DPAT (8-hydroxy-2-(di-n-propylamino)tet-ralin), from rat hippocampal homogenate	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (1998) 8: 2467-2472 [PMID:9873563]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1A receptor of rat hippocampus using [3H]-8-hydroxy-2-(di-n-propylamine) tetralin (8-OH-DPAT) as a radioligand	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1991) 34: 2633-2638 [PMID:1652026]
ChEMBL	Binding affinity towards rat 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT radioligand.	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1996) 39: 4439-4450 [PMID:8893838]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1A receptor in the rat brain (hippocampus) using [3H]8-OH-DPAT	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1996) 39: 1125-1129 [PMID:8676348]
ChEMBL	Binding affinity of compound towards 5-hydroxytryptamine 1A receptor in rat striatal membranes by [3H]OH-DPAT displacement.	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1989) 32: 1921-1926 [PMID:2754715]
ChEMBL	Inhibition of binding of [125I]8-OH-PIPAT ligand to 5-hydroxytryptamine 1A receptor of rat hippocampal homogenates	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1994) 37: 1406-1407 [PMID:8182697]
ChEMBL	In vitro ability to displace the radioligand [3H]-OH-DPAT from binding to rat 5-hydroxytryptamine 1A receptor	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5863-5866 [PMID:15501057]
ChEMBL	Evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat brain	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1988) 31: 1968-1971 [PMID:3172131]
ChEMBL	Binding affinity at 5-hydroxytryptamine 1A receptor in rat cerebral cortex membranes by [3H]8-OH-DPAT displacement.	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (1996) 6: 689-694
ChEMBL	Binding affinity at 5-hydroxytryptamine 1A receptor in rat cerebral cortex membranes by [3H]8-OH-DPAT displacement.	B	9.22	pKi	0.6	nM	Ki	Bioorg Med Chem Lett (1996) 6: 689-694
ChEMBL	Ability to displace [3H]8-OH-DPAT from 5-hydroxytryptamine 1A receptor	B	9.26	pKi	0.55	nM	Ki	J Med Chem (1999) 42: 4952-4960 [PMID:10585205]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL	Binding affinity at 5-hydroxytryptamine 1B receptor	B	5.97	pKi	1071.52	nM	Ki	J Med Chem (1995) 38: 4044-4055 [PMID:7562940]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL	Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry	B	9.22	pKi	0.6	nM	Ki	Eur J Med Chem (2014) 85: 716-726 [PMID:25128671]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL	In vitro ability to displace the radioligand [3H]5-CT from binding to rat 5-hydroxytryptamine 7 receptor	B	7.06	pKi	87	nM	Ki	Bioorg Med Chem Lett (2004) 14: 5863-5866 [PMID:15501057]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb	-	-	6.7	pKi	-	-	-	Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]

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]