ChEMBL ligand: CHEMBL3577885 (Pf-05105679, PF 5105679)
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] 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
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
ChEMBL	Selectivity interaction (GPCR panel (PDSP screen)) EUB0000304b GABRA1	B	5.99	pKi	1022.12	nM	Ki	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibition of dofetilide binding to human ERG	B	4.8	pKi	>15857	nM	Ki	ACS Med Chem Lett (2015) 6: 419-424 [PMID:25893043]
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7]
ChEMBL	Cold activation	B	6.32	pIC50	480	nM	IC50	Data for DCP probe PF-05105679
ChEMBL	Antagonist activity against human recombinant TRPM8 expressed in CHO T-rex cells assessed as inhibition of WS12-induced calcium response pre-incubated for 20 mins before WS12 addition	B	6.74	pIC50	181	nM	IC50	ACS Med Chem Lett (2015) 6: 419-424 [PMID:25893043]
ChEMBL	WS-12 ((2S,5R)-2-isopropyl-N-(4-methoxyphenyl)-5-methylcyclohexanecarboximide) agonist activation	B	6.74	pIC50	181	nM	IC50	Data for DCP probe PF-05105679
ChEMBL	Affinity Biochemical interaction (FLIPR assay) EUB0000304b TRPM8	B	6.74	pIC50	181	nM	IC50	Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Affinity On-target Cellular interaction (Clamp electrophysiology (Ephys) assay (inhibition of voltage-induced current in HEK-293 cells expressing human TRPM8 channel)) EUB0000304b TRPM8	B	6.99	pIC50	103	nM	IC50	Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Voltage activation at room temperature	B	6.99	pIC50	103	nM	IC50	Data for DCP probe PF-05105679
ChEMBL	Antagonist activity against human TRPM8 by single cell patch clamp electrophysiology	B	6.99	pIC50	103	nM	IC50	ACS Med Chem Lett (2015) 6: 419-424 [PMID:25893043]
GtoPdb	-	-	6.99	pIC50	103	nM	IC50	ACS Med Chem Lett (2015) 6: 419-24 [PMID:25893043]
ChEMBL	Transients WS-12 activation	B	7.53	pIC50	29.6	nM	IC50	Data for DCP probe PF-05105679
ChEMBL	Selectivity interaction (Voltage activation assay (using HEK-293 cells at 12°C)) EUB0000304b TRPM8	B	7.86	pIC50	13.8	nM	IC50	Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL	Voltage activation at 12 °C	B	7.86	pIC50	13.8	nM	IC50	Data for DCP probe PF-05105679

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]