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Compound Detail

CHEMBL200469

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CC(=O)c1ccc(NC(=O)c2cn[nH]c2-c2cc(Cl)c(O)cc2O)cc1

Basic Information

ChEMBL ID CHEMBL200469
Phase Preclinical
Structure Type MOL
InChI Key BTTFXKUTBNGQTP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

371.8
MW (Da)
3.60
ALogP
5
HBA
4
HBD
115.3
PSA (Ų)
0.52
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C18H14ClN3O4
MW 371.78
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.03

Activity Summary

IC50 2 meas. best 6.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Heat shock protein HSP90
CHEMBL2095165
IC50 6.59 6.59 258.0 1
Heat shock protein HSP 90-beta
CHEMBL4303
IC50 6.59 6.59 258.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Heat shock protein HSP90 IC50 = 258.0 nM 6.59 Binding affinity to Hsp90 by fluorescent polarization assay 16213716
Heat shock protein HSP 90-beta IC50 = 258.0 nM 6.59 Inhibition of Hsp90 19017562

Literature References

PubMed DOI Target Context # Activities
16213716 10.1016/j.bmcl.2005.08.091 Heat shock protein HSP90 1
16213716 10.1016/j.bmcl.2005.08.091 HCT-116 1
19017562 10.1016/j.bmc.2008.10.087 Heat shock protein HSP 90-beta 1
19017562 10.1016/j.bmc.2008.10.087 HCT-116 1

Data from ChEMBL 36 via Core Engine