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	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	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	Displacement of [3H]-8-OH-DPAT from rat hippocampus 5-HT1A receptor by liquid scintillation counting analysis	B	9.22	pKi	0.6	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
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	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 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	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-CT from human 5-HT7b receptor expressed in HEK293 cells incubated for 1 hr by microbeta plate reader analysis	B	7.06	pKi	87	nM	Ki	Eur J Med Chem (2022) 227: 113931-113931 [PMID:34710746]
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 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]