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Compound Detail

CHEMBL4799160

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Cc1c(C(F)(C(F)(F)F)C(F)(F)F)ccc2c1CC[C@H]1N(C(=O)[C@H]3CC[C@H](C(=O)O)CC3)CC[C@@]21S(=O)(=O)c1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL4799160
Phase Preclinical
Structure Type MOL
InChI Key OCCWVQWCVNDRKB-BKNJMBQISA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
2
Publications
0
Known Names

Molecular Properties

667.6
MW (Da)
6.53
ALogP
4
HBA
1
HBD
91.8
PSA (Ų)
0.29
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H29F8NO5S
MW 667.62
Aromatic Rings 2
Heavy Atoms 45
NP-Likeness -0.35

Activity Summary

EC50 1 meas. best 6.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nuclear receptor ROR-gamma
CHEMBL1741186
EC50 6.06 6.06 870.0 1

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - Homo sapiens
t1/2 - - Mus musculus
t1/2 - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nuclear receptor ROR-gamma EC50 = 870.0 nM 6.06 Inverse agonist activity at Gal4-fused RORgammat (unknown origin) 32882417

Literature References

PubMed DOI Target Context # Activities
32882417 10.1016/j.bmcl.2020.127521 ADMET 3
32882417 10.1016/j.bmcl.2020.127521 Nuclear receptor ROR-gamma 2

Data from ChEMBL 36 via Core Engine