MSD-M1PAM

2D structure
Target CHRM1 
Mode of action Positive allosteric modulator
Control MSD-M1PAM-NC
Recommended cellular usage concentration < 1 µM
In vivo use Yes
Synonyms M1PAM, PQCA
Donated by MSD


Probe criteria


Inhibitor/agonist potency: goal is < 100 nM (IC50, Kd) N/A
Selectivity within target family: > 30-fold Surpasses criterion: > 700-fold selectivity over CHRM2, CHRM3, CHRM4
Clean PDSP scan
Selectivity outside target family Closest off-targets (Panlabs): PTPN2: IC50 = 10 µM @ 10 µM;
On target cell activity for cell-based targets: goal is < 1 µM IC50/EC50 Surpasses criterion: CHRM1: Inflection point = 136 nM (Fold potentiation assay with CHONFATcells expressing human mAChR1 receptor)
Control compound (100 times less potent than the probe) Surpasses criterion: Inflection point for CHRM1 > 10000 µM
Clean PDSP scan