Compound name
TP-021
Protein family
Apoptosis regulator
Target name
BCL6
Affinity biochemical (nM)
100
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000316c
SMILES
O=C1CCc2cc(Nc3cc(OC4CCOCC4)c([N+](=O)[O-])cc3Cl)ccc2N1
InChIKey
RRELDGDKULRRDM-UHFFFAOYSA-N
NCBI gene ID
604
UniProt ID
P41182
Synonyms
BCL6, BCL5, LAZ3, ZBTB27, ZNF51
Mode of action
Inhibitor
Negative control
TP-021n
Affinity biochemical definition
IC50
Affinity biochemical assay type
Cell-free enzyme-linked immunosorbent assay (ELISA)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-021
https://doi.org/10.1016/j.bmc.2017.07.037
Affinity biochemical relation
=
Selectivity platform
KinomeScan (DiscoverX)
Selectivity platform number of targets
468
Selectivity remarks
Screened at 1 µM, closest targets as % of contrl.: NEK1 (40%), STK38L (41%), EIF2AK2 (46%); Screen against 45 GPCR targets (PDSP screen) at 10 µM, closest target as % inhibition: CHRM4 (49%); Clean in Takeda in-house kinase panel against 344 targets, at 1 µM; compound is protein-protein inhibitor targetting non-conserved sites.
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-021
https://doi.org/10.1016/j.bmc.2017.07.037
Selectivity Number of Off-targets
0