Compound name
BI 653048
Protein family
Nuclear Receptor
Target name
NR3C1
Affinity biochemical (nM)
55
Affinity on-target cellular (nM)
23
CG-Set
NR set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000314c
SMILES
CCS(c1cc2cc(C[C@](CC(C)(C)c3ccc(cc3C(N)=O)F)(C(F)(F)F)O)[nH]c2cn1)(=O)=O
InChIKey
CYFBRQHYEQKYHH-MRXNPFEDSA-N
NCBI gene ID
2908
UniProt ID
P04150
Synonyms
GR
Mode of action
Agonist
Negative control
BI-3047
Affinity biochemical definition
IC50
Affinity biochemical assay type
Fluorescence polarization assay
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/25516791/
Affinity biochemical relation
0
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
Fibroblast IL-6 assay (suppression of IL-1 induced IL-6 production in human foreskin fibroblasts)
Affinity on-target cellular source knowledge
https://pubmed.ncbi.nlm.nih.gov/25516791/
Affinity on-target cellular relation
0
Selectivity platform
Eurofins-Panlabs screen
Selectivity platform number of targets
49
Selectivity remarks
Screened at 10 µM; >100 fold selective against related nuclear receptors (PGR, NR3C2, ESR1, AR); Screened at 10 µM against 45 GPCRs, closest targets >30% of inhibition: DRD5 (34%), HTR3A (32%); Screened at 1 µM against 468 kinases (KinomeScan, DiscoverX), closest targets <45% of control: LATS2 (40%), NDR2 (45%), NEK1 (45%)
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/BI%20653048
Selectivity Number of Off-targets
0