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Compound Detail

CHEMBL3235342

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CN1CCc2c3c(n(-c4ccc(C(N)=O)c(NCC5(C)COC5)c4)c2C1)CC(C)(C)CC3=O

Basic Information

ChEMBL ID CHEMBL3235342
Phase Preclinical
Structure Type MOL
InChI Key BBERRDWXGILBQQ-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

450.6
MW (Da)
3.17
ALogP
6
HBA
2
HBD
89.6
PSA (Ų)
0.73
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 C26H34N4O3
MW 450.58
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.55

Activity Summary

Ki 4 meas. best 7.66
IC50 1 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Heat shock protein HSP 90-beta
CHEMBL4303
Ki 7.66 7.66 22.0 1
Heat shock protein HSP 90-alpha
CHEMBL3880
Ki 7.55 7.55 28.0 1
Heat shock protein HSP 90-beta
CHEMBL4303
IC50 6.35 6.35 450.0 1
Endoplasmin
CHEMBL1075323
Ki 6.21 6.21 620.0 1
Heat shock protein 75 kDa, mitochondrial
CHEMBL1075132
Ki 5.92 5.92 1200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24673104 10.1021/jm500042s Heat shock protein HSP 90-beta 2
24673104 10.1021/jm500042s Heat shock protein HSP 90-alpha 1
24673104 10.1021/jm500042s Endoplasmin 1
24673104 10.1021/jm500042s Heat shock protein 75 kDa, mitochondrial 1

Data from ChEMBL 36 via Core Engine