Compound name
AX-15836
Protein family
Protein Kinase
Target name
MAPK7
Affinity biochemical (nM)
8
Affinity on-target cellular (nM)
9
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0003009a
SMILES
O=C1N(C)C2=CN=C(NC3=CC=C(C(N4CCC(N5CCN(C)CC5)CC4)=O)C=C3OCC)N=C2N(S(=O)(C)=O)C6=CC=CC=C16
InChIKey
HTFNVAVTYILUCF-UHFFFAOYSA-N
NCBI gene ID
5598
UniProt ID
Q13164
Synonyms
BMK1, ERK5
Mode of action
Inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzymatic assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/27679845/
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Cellular assay (KiNative using HUVEC cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/27679845/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (KiNative chemoproteomics profiling, Jurkat cells)
Selectivity platform number of targets
>200
Selectivity remarks
Screened at 1 µM, closest targets as % of inhibition: MAPK7 (99.2%), SRPK1 (35%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27679845/;
Screened at 10 µM, Kinase panel (KiNative chemoproteomics profiling, Jurkat cells), >200 kinases, closest targets as % of inhibition: MAPK7 (96.1%), NLK1 (41.7%), CDK7 (40.1%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27679845/;
Screened at 10 µM, Kinase panel (KiNative chemoproteomics profiling, Jurkat cells), >200 kinases, closest targets as % of inhibition: MAPK7 (96.1%), NLK1 (41.7%), CDK7 (40.1%), full screening data are available as supporting information, https://pubmed.ncbi.nlm.nih.gov/27679845/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/27679845/
Selectivity Number of Off-targets
0