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Compound Detail

CHEMBL147845

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Cc1cc2c(cc1-c1cc(C(=O)O)no1)C(C)(C)C(C)CC2(C)C

Basic Information

ChEMBL ID CHEMBL147845
Phase Preclinical
Structure Type MOL
InChI Key UWSDSQVGPVPJRF-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

327.4
MW (Da)
4.94
ALogP
3
HBA
1
HBD
63.3
PSA (Ų)
0.85
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H25NO3
MW 327.42
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -0.01

Activity Summary

IC50 1 meas. best 4.14
Kd 1 meas. best 5.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor gamma
CHEMBL2003
Kd 5.21 5.21 6100.0 1
HL-60
CHEMBL383
IC50 4.14 4.14 73000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Retinoic acid receptor gamma Kd = 6100.0 nM 5.21 In vitro binding affinity for Retinoic acid receptor RAR gamma 10585206
HL-60 IC50 = 73000.0 nM 4.14 Cytostatic activity against HL-60 cells 10585206

Literature References

PubMed DOI Target Context # Activities
10585206 10.1021/jm991059n HL-60 4
10585206 10.1021/jm991059n Retinoic acid receptor RXR-alpha 2
10585206 10.1021/jm991059n Retinoic acid receptor RXR-beta 2
10585206 10.1021/jm991059n Retinoic acid receptor RXR-gamma 2
10585206 10.1021/jm991059n Retinoic acid receptor alpha 2
10585206 10.1021/jm991059n Retinoic acid receptor beta 2
10585206 10.1021/jm991059n Retinoic acid receptor gamma 2

Data from ChEMBL 36 via Core Engine