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Table 8BComparative Downstream and Selectivity assays by Assay Provider for CID1542103

Image ml145fu22.jpg
GPR35
AID-2480
pERK-ICW
AID-463217
Vasopressin IIa Agonist
AID-463201

%Activation @ 10 µM
Vaopressin IIa Antagonist
AID-463202

%Inhibition @ 10 µM
CIDSIDR1R2IC50 (µM)IC50(µM)n
1542103*875444962-Me4-Cl4.72>3290.0/−0.3; Avg. −0.1613.6/1.6; Avg. 7.6
1502520*875444972-Me4-Me5.0117.7 ±0.109−0.4/0.2; Avg. −0.0840.4/33.3; Avg. 36.9
8056691*87544526H4-Cl9.76>3250.3/−0.4; Avg. −0.08−42.7/49.5; Avg. 3.4
805664187544527HHNot potent in GPR35 Primary assay so not tested for the downstream assays.
661907875445234-Me4-MeNot potent in GPR35 Primary assay so not tested for the downstream assays.
2474060875445374-F2,4-ClNot potent in GPR35 Primary assay so not tested for the downstream assays.
*

Clear solution at 10 mM nominal in DMSO

Clear solution at 10 mM nominal in DMSO

From: Selective GPR35 Antagonists - Probes 1 & 2

Cover of Probe Reports from the NIH Molecular Libraries Program
Probe Reports from the NIH Molecular Libraries Program [Internet].

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