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Compound Detail

CHEMBL139536

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COC(=O)c1ccc(C(=O)Nc2ccc3c(c2)C(C)(C)CC(C)(C)S3)cc1

Basic Information

ChEMBL ID CHEMBL139536
Phase Preclinical
Structure Type MOL
InChI Key JZHWLPKXASYCHY-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

383.5
MW (Da)
5.28
ALogP
4
HBA
1
HBD
55.4
PSA (Ų)
0.73
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25NO3S
MW 383.51
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.65

Activity Summary

EC50 6 meas. best 7.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-beta
CHEMBL4047
EC50 7.17 7.17 68.0 1
Retinoic acid receptor RXR-alpha
CHEMBL3084
EC50 7.08 7.08 84.0 1
Retinoic acid receptor gamma
CHEMBL2003
EC50 6.82 6.82 152.0 1
Retinoic acid receptor alpha
CHEMBL2055
EC50 6.65 6.65 225.0 1
Retinoic acid receptor RXR-gamma
CHEMBL4402
EC50 6.52 6.52 302.0 1
Retinoic acid receptor beta
CHEMBL2008
EC50 6.0 6.0 1004.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10543887 10.1021/jm990292i SCC-2 1
10543887 10.1021/jm990292i SCC-38 1
10543887 10.1021/jm990292i Retinoic acid receptor alpha 1
10543887 10.1021/jm990292i Retinoic acid receptor beta 1
10543887 10.1021/jm990292i Retinoic acid receptor gamma 1
10543887 10.1021/jm990292i Retinoic acid receptor RXR-alpha 1
10543887 10.1021/jm990292i Retinoic acid receptor RXR-beta 1
10543887 10.1021/jm990292i Retinoic acid receptor RXR-gamma 1

Data from ChEMBL 36 via Core Engine