Compound name
M4K2234
Protein family
Protein Kinase
Target name
ACVR1
Affinity biochemical (nM)
14
Affinity on-target cellular (nM)
13
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0001184b
SMILES
COc1cc(-c2cncc(-c3ccc(N4CCN(C(C)C)CC4)cc3)c2C)cc(F)c1C(N)=O
InChIKey
RIWTUJFFSTVYPW-UHFFFAOYSA-N
NCBI gene ID
90
UniProt ID
Q04771
Synonyms
SKR1, ALK2, ACVR1A
Mode of action
inhibitor
Negative control
M4K2234NC
Affinity biochemical definition
IC50
Affinity biochemical assay type
Radiometric assay and ³³PanQinase™
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/m4k2234
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
NanoBRET assay (HEK293T cells)
Affinity on-target cellular source knowledge
https://www.thesgc.org/chemical-probes/m4k2234
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Reaction Biology)
Selectivity platform number of targets
375
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: TNIK (4.92%), ALK6 (27%), MAP4K4 (30%); In-vitro follow-up of closest targets and ALK family (biochemical assays, Reaction Biology, 10 mM ATP): IC50(ALK3) = 168 nM, IC50(ALK4) = 1660 nM, IC50(ALK5) 1950 nM, IC50(ALK6) = 88 nM, IC50(TNIK) = 41 nM; In-cellulo potency (NanoBRET assay in HEK293T cells): IC50(ALK3) = 536 nM, IC50(ALK4) = 8424 nM, IC50(ALK5) = 7932 nM, IC560(ALK6) = 1628 nM, https://www.thesgc.org/chemical-probes/m4k2234;
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/m4k2234