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Compound Detail

CHEMBL1917462

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Cc1c(Sc2ccc(Cl)cc2)c2c(Cl)nccc2n1CC(=O)O

Basic Information

ChEMBL ID CHEMBL1917462
Phase Preclinical
Structure Type MOL
InChI Key XEYDGQLGRXJVCH-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

367.3
MW (Da)
4.89
ALogP
4
HBA
1
HBD
55.1
PSA (Ų)
0.67
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H12Cl2N2O2S
MW 367.26
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.26

Activity Summary

IC50 1 meas. best 7.5
Ki 1 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prostaglandin D2 receptor 2
CHEMBL5071
IC50 7.5 7.5 32.0 1
Prostaglandin D2 receptor 2
CHEMBL5071
Ki 7.24 7.24 58.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prostaglandin D2 receptor 2 IC50 = 32.0 nM 7.5 Displacement of [3H]PGD2 from human CRTH2 receptor 21944852
Prostaglandin D2 receptor 2 Ki = 58.0 nM 7.24 Inhibition of CRTH2 22224640

Literature References

PubMed DOI Target Context # Activities
21944852 10.1016/j.bmcl.2011.08.124 Prostaglandin D2 receptor 2 1
21944852 10.1016/j.bmcl.2011.08.124 No relevant target 1
22224640 10.1021/jm2013997 Prostaglandin D2 receptor 2 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine