ChEMBL ligand: CHEMBL490153
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor subunit alpha-7 in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544] There should be some charts here, you may need to enable JavaScript!
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] 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
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor subunit alpha-7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
ChEMBL	Positive allosteric modulation at human alpha7 nACHR expressed in Xenopus oocyte assessed as potentiation of 200 uM ACh-induced current at holding potential of -80 mV by electrophysiology	B	5.96	pEC50	1100	nM	EC50	Eur J Med Chem (2014) 86: 724-739 [PMID:25232969]
ChEMBL	Allosteric modulator activity at alpha7 nAChR in human IMR32 cells assessed as stimulation of agonist-induced intracellular calcium level by FLIPR assay	F	6	pEC50	1000	nM	EC50	J Med Chem (2009) 52: 3377-3384 [PMID:19419141]
ChEMBL	Agonist activity at recombinant human nAChRalpha7 expressed in HEK293 Flip-In cells co-expressing RIC3 assessed as increase in intra cellular calcium level after 10 mins by fluorescence relative to control	B	6.22	pEC50	600	nM	EC50	Eur J Med Chem (2021) 214: 113189-113189 [PMID:33540354]
ChEMBL	Positive allosteric modulatory activity against alpha7 nAChR in human IMR-32 cells assessed as potentiation of PNU-282987-induced Ca2+ efflux at by FLIPR assay	B	6.67	pEC50	212	nM	EC50	J Med Chem (2020) 63: 944-960 [PMID:31755711]
Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Displacement of [3H]dofetilide from human ERG channel	B	5	pKi	>10000	nM	Ki	J Med Chem (2009) 52: 3377-3384 [PMID:19419141]
ChEMBL	Inhibition of human ERG channel	B	4.7	pIC50	>20000	nM	IC50	J Med Chem (2009) 52: 3377-3384 [PMID:19419141]

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]