Compound name
BI 99179
Protein family
Synthase
Target name
FASN
Affinity biochemical (nM)
79
Affinity on-target cellular (nM)
180
CG-Set
Other targets
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000294b
SMILES
CCC(=O)N[C@H]1CC[C@@H](C(=O)N(C)c2ccc(-c3nc4ccccc4o3)cc2)C1
InChIKey
YNFDIGJKJPNFFD-SJORKVTESA-N
NCBI gene ID
2194
UniProt ID
P49327
Synonyms
FAS, OA-519, SDR27X1
Mode of action
Inhibitor
Negative control
BI 99990
Affinity biochemical definition
IC50
Affinity biochemical assay type
Human FAS enzyme assay (measuring consumption of NADPH)
Affinity Biochemical Source Knowledge
https://doi.org/10.1016/j.bmcl.2011.07.083
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BI%2099179
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Cellular activity assay (inhibition of [14C]acetate incorporation into human H1975 cells)
Affinity on-target cellular relation
=
Selectivity remarks
Screened against 468 kinases (KinomeScan DiscoverX) at 1 µM, closest targets as % of contr.: MAP2K5 (16%), NTRK3 (32%), AURKA (43%), LATS1 (48%); Screened against 30 GPCR, ion channels, receptors and other enzymes (MDS Pharma Service panel, radioligand binding assays) at 10 µM, closest target as % inhibition: Imidazoline I2, central (19%); Screened against 45 GPCRs (PDSP screen) at 10 µM, closest targets: SLC6A3 (77%)
Selectivity Source Knowledge
https://doi.org/10.1016/j.bmcl.2011.07.083
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BI%2099179