ChEMBL ligand: CHEMBL3286580 (Idalopirdina, Idalopirdine, Lu-ae58054, Lu AE58054, LU AE-58054, LU-AE-58054, LU-AE58054, LY-483518, LY483518, SGS-518, SGS518)
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-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] 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 5-HT1A receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis	B	5.4	pKi	3936	nM	Ki	Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Binding affinity to human 5-HT2AR expressed in HEK293 cells by competitive binding assay	B	6.1	pKi	791	nM	Ki	Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022]
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL	Displacement of [3H]5-HT from 5-HT2C receptor (unknown origin) expressed in hamster AV12 cells	B	6.6	pKi	251.19	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
GtoPdb	-	-	6.6	pKi	250	nM	Ki	J Med Chem (2014) 57: 5823-8 [PMID:24878269]
ChEMBL	Displacement of [3H]5-HT from 5-HT2C receptor (unknown origin) expressed in hamster AV12 cells	B	6.6	pKi	250	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
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 HEK293 cell membrane measured after 60 mins	B	8.16	pKi	6.9	nM	Ki	Eur J Med Chem (2021) 210: 113059-113059 [PMID:33310288]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis	B	8.45	pKi	3.54	nM	Ki	Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022]
ChEMBL	Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis	B	9.08	pKi	0.83	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
GtoPdb	-	-	9.08	pKi	0.83	nM	Ki	J Med Chem (2014) 57: 5823-8 [PMID:24878269]
ChEMBL	Binding affinity to 5HT6R (unknown origin)	B	9.08	pKi	0.83	nM	Ki	Eur J Med Chem (2018) 144: 716-729 [PMID:29291439]
ChEMBL	Displacement of [3H]-LSD from human 5HT6 receptor expressed in CHO cells assessed as inhibition constant incubated for 120 mins by liquid scintillation counting analysis	B	9.08	pKi	0.83	nM	Ki	Bioorg Med Chem (2022) 71: 116950-116950 [PMID:35926324]
ChEMBL	Displacement of [3H]-LSD from human 5HT6R expressed in CHO cell membranes incubated for 120 mins by scintillation counter method	B	9.08	pKi	0.83	nM	Ki	Bioorg Med Chem (2022) 70: 116917-116917 [PMID:35839536]
ChEMBL	Binding affinity to 5-HT6R (unknown origin) assessed as inhibition constant	B	9.08	pKi	0.83	nM	Ki	Bioorg Med Chem Lett (2021) 49: 128275-128275 [PMID:34311086]
ChEMBL	Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis	B	9.08	pKi	0.83	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL	Antagonist activity at 5-HT6 receptor (unknown origin)	B	9.08	pKi	0.83	nM	Ki	Bioorg Med Chem (2023) 84: 117256-117256 [PMID:37003157]
ChEMBL	Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells	B	9.08	pKi	0.83	nM	Ki	J Med Chem (2014) 57: 7160-7181 [PMID:24850589]
ChEMBL	Antagonist activity at 5-HT6 receptor (unknown origin)	B	9.08	pKi	0.83	nM	Ki	J Med Chem (2017) 60: 1843-1859 [PMID:28212021]
ChEMBL	Antagonist activity at human 5HT6 receptor expressed in COS-7 cells assessed as inhibition of 5HT-induced cAMP accumulation preincubated for 7 mins followed by 5-HT addition and measured after 10 mins by HTRF assay	F	6	pIC50	1000	nM	IC50	Eur J Med Chem (2021) 210: 113059-113059 [PMID:33310288]
ChEMBL	Antagonist activity at recombinant human 5HT6R expressed in CHO cells assessed as inhibition of 5HT-stimulated cAMP accumulation incubated for 4 hrs by luminescence counter analysis	F	7.59	pIC50	26	nM	IC50	Bioorg Med Chem (2022) 70: 116917-116917 [PMID:35839536]
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	9.08	pKi	0.83	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]-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by microbeta plate reader analysis	B	5.06	pKi	8635	nM	Ki	Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022]
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 D2R expressed in HEK293 cells after 1 hr by microbeta plate reader analysis	B	5.92	pKi	1215	nM	Ki	Eur J Med Chem (2020) 185: 111857-111857 [PMID:31734022]

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]