ChEMBL ligand: CHEMBL1083390 (GSK-742457, GSK742457, Intepirdina, Intepirdine, RVT-101, Sb-742457, SB-742457)
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] There should be some charts here, you may need to enable JavaScript!
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] There should be some charts here, you may need to enable JavaScript!
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Rat [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388] There should be some charts here, you may need to enable JavaScript!
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] There should be some charts here, you may need to enable JavaScript!
D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] 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
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Displacement of [3H]-8-OH-DPAT from human 5HT1AR expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	5.63	pKi	2370	nM	Ki	Eur J Med Chem (2018) 144: 716-729 [PMID:29291439]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Displacement of [3H]-Ketanserin from human 5HT2AR expressed in CHO-K1 cell membranes after 1.5 hrs by microbeta counting method	B	7.59	pKi	26	nM	Ki	Eur J Med Chem (2018) 144: 716-729 [PMID:29291439]
ChEMBL	Displacement of [3H]-ketanserin from human 5-HT2A receptor extracted from CHO-K1 cell membrane by microbeta plate reader analysis	B	7.6	pKi	25.1	nM	Ki	Eur J Med Chem (2024) 275: 116615-116615 [PMID:38936149]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells	B	8	pKi	<10	nM	Ki	Bioorg Med Chem Lett (2009) 19: 3214-3216 [PMID:19433358]
ChEMBL	Displacement of [3H]LSD from human 5-HT6R expressed in HEK293 cell membranes after 1 hr	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem (2018) 26: 3588-3595 [PMID:29853337]
ChEMBL	Displacement of [3H]-LSD from human 5HT-6 receptor expressed in HEK293 cell membranes assessed as inhibition constant measured after 1 hr by microplate reader analysis	B	8.85	pKi	1.4	nM	Ki	J Med Chem (2023) 66: 14928-14947 [PMID:37797083]
ChEMBL	Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cell membranes measured after 1 hr by microbeta counting method	B	8.85	pKi	1.4	nM	Ki	J Med Chem (2021) 64: 13279-13298 [PMID:34467765]
ChEMBL	Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis	B	8.85	pKi	1.4	nM	Ki	J Med Chem (2021) 64: 1180-1196 [PMID:33439019]
ChEMBL	Displacement of [3H]-LSD from human 5HT6R expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	8.85	pKi	1.4	nM	Ki	Eur J Med Chem (2018) 144: 716-729 [PMID:29291439]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6 receptor extracted from HEK293 cell membrane by microbeta plate reader analysis	B	8.89	pKi	1.3	nM	Ki	Eur J Med Chem (2024) 275: 116615-116615 [PMID:38936149]
ChEMBL	Binding affinity to 5HT6R (unknown origin)	B	9.55	pKi	0.28	nM	Ki	Eur J Med Chem (2018) 144: 716-729 [PMID:29291439]
ChEMBL	Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant	B	9.6	pKi	0.25	nM	Ki	Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
ChEMBL	Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells	B	9.6	pKi	0.25	nM	Ki	J Med Chem (2014) 57: 7160-7181 [PMID:24850589]
ChEMBL	Binding affinity to 5HT6 receptor	B	9.63	pKi	0.23	nM	Ki	J Med Chem (2010) 53: 5186-5196 [PMID:20560595]
ChEMBL	Antagonist activity at 5-HT6 receptor (unknown origin)	B	9.64	pKi	0.23	nM	Ki	J Med Chem (2017) 60: 1843-1859 [PMID:28212021]
ChEMBL	Antagonist activity at 5-HT6 receptor (unknown origin)	B	9.64	pKi	0.23	nM	Ki	Bioorg Med Chem (2013) 21: 4614-4627 [PMID:23787290]
ChEMBL	Binding affinity to 5-HT6 receptor (unknown origin)	B	9.77	pKi	0.17	nM	Ki	J Med Chem (2024) 67: 1580-1610 [PMID:38190615]
ChEMBL	Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis	B	9.77	pKi	0.17	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
GtoPdb	HeLa cell membrane assay, displacing [3H]LSD	-	9.77	pKi	0.17	nM	Ki	J Med Chem (2014) 57: 5823-8 [PMID:24878269]
ChEMBL	Displacement of [3H]LSD from human 5-HT6 receptor expressed in human HeLa cells after 1 hr by scintillation spectroscopic analysis	B	9.78	pKi	0.17	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL	Inverse agonist activity at recombinant human 5HT6 receptor expressed in NG108-15 cells assessed as inhibition of cAMP production measured after 5 mins by BRET assay	F	7.01	pIC50	97	nM	IC50	Eur J Med Chem (2020) 208: 112765-112765 [PMID:32949963]
ChEMBL	Antagonist activity at 5HT6R (unknown origin) transfected in NG108-15 cells co-transfected with CAMYEL assessed as reduction in cAMP levels after 5 mins by Coelanterazine H-based BRET assay	F	8.55	pIC50	2.8	nM	IC50	Eur J Med Chem (2018) 144: 716-729 [PMID:29291439]
ChEMBL	Inverse agonist activity at 5HT6R (unknown origin) expressed in 1321N1 cells co-expressing CAMYEL assessed as reduction in basal cAMP accumulation by BRET assay	F	8.55	pIC50	2.8	nM	IC50	J Med Chem (2021) 64: 1180-1196 [PMID:33439019]
ChEMBL	Antagonist activity at 5-HT6 receptor (unknown origin) expressed in NG108-15 cells assessed as reduction in cAMP level after 5 mins by BRET assay	F	8.55	pIC50	2.8	nM	IC50	J Med Chem (2021) 64: 13279-13298 [PMID:34467765]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388]
ChEMBL	Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor	B	9.63	pKi	0.23	nM	Ki	ACS Med Chem Lett (2016) 7: 618-622 [PMID:27326337]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL	Displacement of [3H]-5-CT from human 5HT7BR expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	4.85	pKi	14230	nM	Ki	Eur J Med Chem (2018) 144: 716-729 [PMID:29291439]
D2 receptor/D(2) dopamine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of [3H]-Raclopride from human dopamine D2L receptor expressed in HEK293 cell membranes after 1 hr by microbeta counting method	B	6	pKi	997	nM	Ki	Eur J Med Chem (2018) 144: 716-729 [PMID:29291439]

ChEMBL data shown on this page come from version 36:

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]