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Compound Detail

CHEMBL44078

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Cc1cccc(N(C)c2cc(Cl)nc(SCC(=O)O)n2)c1C

Basic Information

ChEMBL ID CHEMBL44078
Phase Preclinical
Structure Type MOL
InChI Key QPKAYXPTNWRYPX-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

337.8
MW (Da)
3.69
ALogP
5
HBA
1
HBD
66.3
PSA (Ų)
0.51
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H16ClN3O2S
MW 337.83
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.38

Activity Summary

EC50 3 meas. best 5.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Retinoic acid receptor RXR-alpha
CHEMBL2061
EC50 5.55 5.55 2800.0 1
Retinoic acid receptor RXR-beta
CHEMBL1870
EC50 5.26 5.26 5500.0 1
Retinoic acid receptor RXR-gamma
CHEMBL2004
EC50 4.77 4.77 17100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
6502593 10.1021/jm00378a016 Rattus norvegicus 4
30702885 10.1021/acs.jmedchem.8b01848 Retinoic acid receptor RXR-alpha 2
30702885 10.1021/acs.jmedchem.8b01848 Retinoic acid receptor RXR-beta 2
30702885 10.1021/acs.jmedchem.8b01848 Retinoic acid receptor RXR-gamma 2
30702885 10.1021/acs.jmedchem.8b01848 Peroxisome proliferator-activated receptor alpha 1
30702885 10.1021/acs.jmedchem.8b01848 Peroxisome proliferator-activated receptor gamma 1
30702885 10.1021/acs.jmedchem.8b01848 Peroxisome proliferator-activated receptor delta 1
30702885 10.1021/acs.jmedchem.8b01848 HepG2 1

Data from ChEMBL 36 via Core Engine