EUB0000623aCl_MAP3K5

Screened at 1 µM, in-vitro potency of closest targets: IC50(ASK2)= 510 nM, IC50(MEKK1) >10 µM, IC50(TAK1) >10 µM, IC50(IKKB) >10 µM, IC50(ERK1) >10 µM, IC50(JNK1) >10µM, IC50(MAPK14) >10 µM, IC50(GSK3B) >10 µM, IC50(PRKCT) >10 µM; Screened against 12 kinases (Invitrogen, enzymatic assays), in-vitro potency of closest targets: IC50(CDK2) = 0.158 µM, IC50(EGFR) <20 µM, IC50(EPHA3) <20 µM, IC50(ERBB4) <20 µM, IC50(GSK3B) = 0.832 µM, IC50(ITK) = 5.5 µM, IC50(MER) = 6.5 µM, IC50(MAPK14) <20 µM, IC50(PRKAA1) = 13.8 µM, IC50(RET) = 11.5 µM, IC50(ROCK1) = 4.9 µM, IC50(RON) <20 µM, https://pubmed.ncbi.nlm.nih.gov/28291695/; Screened at 20 µM against 100 kinases, DSF panel, closest targets with dTm >5 K: dTm(MAP3K5) = 12.41 K, dTm(CLK1) = 5.46 K, closest targets with dTm 3-5 K: dTm(CAMKK2) = 4.55 K, dTm(RPS6KA5) = 3.13 K, in-house data SGC Frankfurt;