Compound name
MSD-M1PAM
Protein family
GPCR
Target name
CHRM1
Affinity on-target cellular (nM)
136
CG-Set
GPCR set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000252b
SMILES
N#CC1(c2ccccn2)CCN(Cc2cc(C(=O)O)c(=O)n3ccccc23)CC1
InChIKey
RJTJRVASUFIDQM-UHFFFAOYSA-N
NCBI gene ID
1128
UniProt ID
P11229
Mode of action
Positive allosteric modulator
Negative control
CHRM1
Affinity on-target cellular definition
Potentiation inflection oint
Affinity on-target cellular assay type
Fold potentiation assay (addition of EC20 acetylcholine; in human M1 expressing Chinese hamster ovary (CHO) cells; using calcium mobilization readout on a fluorometric imaging plate reader (FLIPR384))
Affinity on-target cellular relation
=
Selectivity platform
GPCR screen (PDSP)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, > 700-fold selective for CHRM2, CHRM3, CHRM4; Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: PIK3CB (36%), TGFBR1 (41%), BLK (49%); Panlabs screen at 10 µM against 140 targets, closest target: IC50( PTPN2) = 10 µM;
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/MSD-M1PAM
Selectivity Number of Off-targets
0