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Compound Detail

CHEMBL4796520

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CCCc1cc2cc(-n3nc(C)c4c3CC(C)(C)CC4=O)cc(N[C@H]3CC[C@H](O)CC3)c2c(=O)[nH]1

Basic Information

ChEMBL ID CHEMBL4796520
Phase Preclinical
Structure Type MOL
InChI Key QRUAXSIQUFUVJC-XGAFWQRZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

476.6
MW (Da)
4.85
ALogP
6
HBA
3
HBD
100.0
PSA (Ų)
0.49
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H36N4O3
MW 476.62
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.69

Activity Summary

IC50 2 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Heat shock protein HSP 90-beta
CHEMBL4303
IC50 7.4 7.4 40.0 1
Heat shock protein HSP 90-alpha
CHEMBL3880
IC50 6.05 6.05 886.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33428418 10.1021/acs.jmedchem.0c01700 Heat shock protein HSP 90-beta 6
33428418 10.1021/acs.jmedchem.0c01700 Heat shock protein HSP 90-alpha 2
33428418 10.1021/acs.jmedchem.0c01700 Unchecked 2
33428418 10.1021/acs.jmedchem.0c01700 Panel NCI-60 (60 carcinoma cell lines) 1
33428418 10.1021/acs.jmedchem.0c01700 UMUC3 1
33428418 10.1021/acs.jmedchem.0c01700 T-24 1
33428418 10.1021/acs.jmedchem.0c01700 PC-3 1
33428418 10.1021/acs.jmedchem.0c01700 LNCaP C4-2B 1
33428418 10.1021/acs.jmedchem.0c01700 LAPC4 1

Data from ChEMBL 36 via Core Engine