Compound name
TP-008
Protein family
Protein Kinase
Target name
TGFBR1
Affinity biochemical (nM)
25
Affinity on-target cellular (nM)
245
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000312b
SMILES
Cc1ncc(-c2cc(Cl)ccc2F)cc1-n1c(=O)n(CC(N)=O)c2cnccc21
InChIKey
HSCQDYRIKMDIJX-UHFFFAOYSA-N
NCBI gene ID
7046
UniProt ID
P36897
Synonyms
ALK-5, ACVRLK4, ALK5, TBRI, TBR-i
Mode of action
Inhibitor
Negative control
Al11
Affinity biochemical definition
IC50
Affinity biochemical assay type
Lathascreen (Takeda)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-008
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Reporter gene assay
Affinity on-target cellular relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
70
Selectivity remarks
Screened at 1 µM, closest targets as % contr.: PIK3CA (33.9%), DDR1 (36.7%), JAK1 (38.6%), PNCK (39.5%), MAPK9 (39.6%), all >20 µM in NanoBRET cellular assays (HEK293T cells)
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-008
Selectivity Number of Off-targets
0