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Compound Detail

CHEMBL5270756

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CC1(C)[C@@H]2CC[C@]1(c1ccnc(N3CCCCC3)n1)c1nnc(-c3c(F)cccc3F)cc12

Basic Information

ChEMBL ID CHEMBL5270756
Phase Preclinical
Structure Type MOL
InChI Key QOYRNTUBIHWFHV-QUGAMOGWSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

447.5
MW (Da)
5.41
ALogP
5
HBA
0
HBD
54.8
PSA (Ų)
0.54
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27F2N5
MW 447.53
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.52

Activity Summary

IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nuclear receptor ROR-gamma
CHEMBL1741186
IC50 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nuclear receptor ROR-gamma IC50 = 2.0 nM 8.7 Inhibition of human RORgamma by TR-FRET assay 30010338

Literature References

PubMed DOI Target Context # Activities
30010338 10.1021/acs.jmedchem.8b00588 Nuclear receptor ROR-gamma 1

Data from ChEMBL 36 via Core Engine