Compound name
BLU-9931
Protein family
Protein Kinase
Target name
FGFR4
Affinity biochemical (nM)
3
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001084a
SMILES
C=CC(=O)Nc1cccc(C)c1Nc1ncc2cc(-c3c(Cl)c(OC)cc(OC)c3Cl)ccc2n1
InChIKey
TXEBNKKOLVBTFK-UHFFFAOYSA-N
NCBI gene ID
2264
UniProt ID
P22455
Synonyms
JTK2, CD334
Mode of action
Covalent inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzyme inhibition assay (conc. ATP = Km)
Affinity Biochemical Source Knowledge
https://aacrjournals.org/cancerdiscovery/article/5/4/424/4943/First-Selective-Small-Molecule-Inhibitor-of-FGFR4
Affinity biochemical relation
=
Selectivity platform
KINOMEscan (DiscoverX)
Selectivity platform number of targets
456
Selectivity remarks
Screened at 3 µM, in-vitro potency of closest target: Kd(CSF1R) = 2716 nM (90.1% inhibition), S-score(10) = 0.005 at 3 µM; In-vitro potencies of other FGFR family members (enzyme activity assays): IC50(FGFR1) = 591 nM, IC50(FGFR2) = 493 nM, IC50(FGFR3) = 150 nM; IC50(p70S6Kb) > 10 μM (https://aacr.silverchair-cdn.com/aacr/content_public/journal/cancerdiscovery/5/4/10.1158_2159-8290.cd-14-1029/4/21598290cd141029-sup-137537_2_supp_0_njmz90.pdf?Expires=1675264845&Signature=C7J4HfbPNEkAbAqzPJ39H9yL-DM-ZriAd8q9~z8YUG1gWwYiv~YY3KnIOiETJu6s6ant4xiTBoYwoCLgll18xYBmbGpqFihOfhV-o13a7i6vEvF1O1eaowwAMUXKijlCNqDlMeXH0BaQ1JGUfaWJ-rcaUZdvfAS~UHg~9yVyE3t7x2JTKWLV3T1OQ0xNVih6dxAH~ACl87xwuIVD4NVAlkEcGUWPGXNzCUzk8-SlPnWgBxnUZLP6R8NhMbrjeOlLoYg0TNe9HVYyYuOCI6bAajPrnqSaYv1qC1eoQq-HWafjwJ7N3T5waFSlCi~COA3D0QYQ~UdoNRFASuZZzqG1Lg__&Key-Pair-Id=APKAIE5G5CRDK6RD3PGA)
Selectivity Source Knowledge
https://aacrjournals.org/cancerdiscovery/article/5/4/424/4943/First-Selective-Small-Molecule-Inhibitor-of-FGFR4
Selectivity Number of Off-targets
0