Compound name
BI-0319
Protein family
Protein Kinase
Target name
PTK2
Affinity biochemical (nM)
20
Affinity on-target cellular (nM)
199
CG-Set
Kinase set
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0001698a
SMILES
COc1cc(C(=O)NCCOCCOCCOCC(=O)N[C@H](C(=O)N2C[C@H](O)C[C@H]2C(=O)NCc2ccc(-c3scnc3C)cc2)C(C)(C)C)ccc1Nc1ncc(C(F)(F)F)c(Oc2cccc3c2C(=O)CC3)n1
InChIKey
UVVQLQQNGHYTOL-JIVXZRRKSA-N
NCBI gene ID
5747
UniProt ID
Q05397
Synonyms
FAK, FADK, FAK1, PPP1R71
Mode of action
Protac
Negative control
BI-4206
Affinity biochemical definition
IC50
Affinity biochemical assay type
Z´-Light assay (Thermo Fisher SelectScreen Kinase Profiling Services, conc. ATP = Km)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/30739444/
Affinity biochemical relation
=
Affinity on-target cellular definition
DC50
Affinity on-target cellular assay type
Protein capillary electrophoresis (Degradation activity using A549 cells, 18h treatment)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/30739444/
Affinity on-target cellular relation
=
Selectivity platform
Kinase panel (Invitrogen)
Selectivity platform number of targets
396
Selectivity remarks
Screened at 1 µM, closest targets as % of control: LRRK2 (4%), LRRK2 (fl, 3%), PTK2 (-0.5%), full screening data available on OpenMe website, https://www.opnme.com/molecules/ptk2-protac-bi-0319; Screened at 1 µM against 397 kinases (Kinase selectivity panels, Thermo Fischer SelectScreen Kinase Profiling Services), closest target >90 % of control: LRRK2, https://pubmed.ncbi.nlm.nih.gov/30739444/; Proteomics at 3 µM, using A549 cells treated for 18h, closest target (protein capillary electrophoresis): EC50 (PDE6D) >1 µM, https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b01826; Screened at 10 µM against 44 other enzymes (SafetyScreen44™, GPCRS, ion channels, hydrolases), closest targets as % of control: CA+/DHPSI/R (Voltage-gated ion channel, 32%), DELTA2/H (GPCR, 35%), full screening data available on OpenMe website, https://www.opnme.com/molecules/ptk2-protac-bi-0319;
Selectivity Source Knowledge
https://www.opnme.com/molecules/ptk2-protac-bi-0319
Selectivity Number of Off-targets
1