Compound name
CCT369260
Protein family
Apoptosis regulator
Target name
BCL6
Affinity biochemical (nM)
520
Affinity on-target cellular (nM)
90
CG-Set
Other targets set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002206a
SMILES
C[C@H]1CN(c2ncc(Cl)c(Nc3ccc4c(c3)n(CCC(C)(C)O)c(=O)n4C)n2)C[C@@H](C)C1(F)F
InChIKey
VFNPUAOAEFMXQI-GASCZTMLSA-N
NCBI gene ID
604
UniProt ID
P41182
Synonyms
BCL6, BCL5, LAZ3, ZBTB27, ZNF51
Mode of action
degrader
Negative control
CCT393732
Affinity biochemical definition
IC50
Affinity biochemical assay type
TR-FRET assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/32275432/
Affinity biochemical relation
0
Affinity on-target cellular definition
DC50
Affinity on-target cellular assay type
Immunofluorescence-based BCL6 degradation assay (in SUDHL-4 cells)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/32275432/
Affinity on-target cellular relation
0
Selectivity platform
GPCR panel (PDSP screen)
Selectivity platform number of targets
45
Selectivity remarks
Screened at 10 µM, closest targets as % of inhibition: OPRM1 (86%), GABA/PBR (59.57%), ADORA1 (93.08%), HRH3 (60.67%), TMEM97 (85.65%), ADRB3 (65.27%), SLC6A3 (50.76%), HTR1D (56.54%), AVPR1A (78.62%), SIGMAR1 (47.38%); In-vitro potency (enzymatic assay): Ki(OPRM1) = 872.47 nM, Ki(GABA/PBR) = 1113.88 nM, Ki(ADORA1) = 1630.55 nM, Ki(HRH3) = 2333.56 nM, Ki(TMEM97) = 2503.46 nM, Ki(ADRB3) = 3994.88 nM, Ki(SLC6A3) = 5087.69 nM, Ki(HTR1D) = 6174.88 nM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!gpcrscandataview/CCT369260
Selectivity Number of Off-targets
1