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Compound Detail

CHEMBL4761001

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CN(C)C/C=C/C(=O)Nc1ccc(C(=O)N2CCCC(Nc3ncc(SCc4ncc(C(C)(C)C)o4)s3)C2)cc1

Basic Information

ChEMBL ID CHEMBL4761001
Phase Preclinical
Structure Type MOL
InChI Key LRXFEHJUJZDISP-VQHVLOKHSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

582.8
MW (Da)
5.49
ALogP
9
HBA
2
HBD
103.6
PSA (Ų)
0.24
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H38N6O3S2
MW 582.80
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -1.54

Activity Summary

IC50 3 meas. best 7.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 9
CHEMBL3116
IC50 7.19 7.19 65.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.04 7.04 92.3 1
Cyclin-dependent kinase 7
CHEMBL3055
IC50 5.3 5.3 5000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 9 IC50 = 65.0 nM 7.19 Inhibition of CDK9 (unknown origin) -
Cyclin-dependent kinase 2 IC50 = 92.3 nM 7.04 Inhibition of CDK2 (unknown origin) -
Cyclin-dependent kinase 7 IC50 = 5000.0 nM 5.3 Inhibition of CDK7 (unknown origin) -

Data from ChEMBL 36 via Core Engine