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Compound Detail

CHEMBL4171515

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Cc1c2c(n(-c3ccc(CC(=O)O)cc3)c1C)CCC(F)(F)C2

Basic Information

ChEMBL ID CHEMBL4171515
Phase Preclinical
Structure Type MOL
InChI Key HGCBSPPZJAZLDQ-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

319.4
MW (Da)
3.85
ALogP
2
HBA
1
HBD
42.2
PSA (Ų)
0.93
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H19F2NO2
MW 319.35
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -0.38

Activity Summary

EC50 3 meas. best 6.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha
CHEMBL2061
EC50 6.01 6.01 970.0 1
Retinoic acid receptor RXR-gamma
CHEMBL2004
EC50 5.47 5.47 3400.0 1
Retinoic acid receptor RXR-beta
CHEMBL1870
EC50 5.35 5.35 4500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29901398 10.1021/acs.jmedchem.8b00494 Retinoic acid receptor RXR-alpha 2
29901398 10.1021/acs.jmedchem.8b00494 Retinoic acid receptor RXR-beta 2
29901398 10.1021/acs.jmedchem.8b00494 Retinoic acid receptor RXR-gamma 2
29901398 10.1021/acs.jmedchem.8b00494 Retinoid X receptor 2

Data from ChEMBL 36 via Core Engine