Compound name
TP-008
Protein family
Protein Kinase
Target name
ACVR1B
Affinity biochemical (nM)
126
Affinity on-target cellular (nM)
526
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
91
UniProt ID
P36896
Synonyms
ALK4, SKR2, ActRIB
Mode of action
Inhibitor
Negative control
Al11
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radioactive kinase assay (ACVR1B)
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