Compound name
PF-05105679
Protein family
TRP channel
Target name
TRPM8
Affinity biochemical (nM)
181
Affinity on-target cellular (nM)
103
CG-Set
Ion Channel
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000304b
SMILES
C[C@H](c1ccc(F)cc1)N(Cc1cccc(C(=O)O)c1)C(=O)c1cnc2ccccc2c1
InChIKey
BXNMZRPTQFVRFA-QGZVFWFLSA-N
NCBI gene ID
79054
UniProt ID
Q7Z2W7
Synonyms
TRPM8, LTRPC6, TRPP8
Mode of action
Antagonist
Negative control
PF-05257137
Affinity biochemical definition
IC50
Affinity biochemical assay type
FLIPR assay
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/ml500479v
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-05105679
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Clamp electrophysiology (Ephys) assay (inhibition of voltage-induced current in HEK-293 cells expressing human TRPM8 channel)
Affinity on-target cellular relation
=
Selectivity platform
CEREP Wide Ligand screening panel, literature
Selectivity platform number of targets
90
Selectivity remarks
Screened at 10 µM, panel of ion channels, receptors, enzymes, > 100-fold selective (including closely related TRPV1, TRPA1 channels); Clean in CardiacProfiler ion channel panel (Millipore) at 10 µM; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: MAPK14 (0%), GRK3 (40%), TAOK3 (41%), PIK3CA(Q546K) (42%); Screened against 45 GPCR targets (PDSP screen) at 10 µM, closest target: Ki (GABA/PBR) = 1022.12 nM
Selectivity Source Knowledge
https://doi.org/10.1021/ml500479v
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/PF-05105679
Selectivity Number of Off-targets
0