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Compound Detail

CHEMBL4468670

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C=CC(=O)Nc1cccc(Nc2cc(N3CCCC[C@H]3CCO)nc3c(CC)cnn23)c1

Basic Information

ChEMBL ID CHEMBL4468670
Phase Preclinical
Structure Type MOL
InChI Key CDCHESFKYUNJPV-FQEVSTJZSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

434.5
MW (Da)
3.90
ALogP
7
HBA
3
HBD
94.8
PSA (Ų)
0.47
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30N6O2
MW 434.54
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.14

Activity Summary

IC50 6 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK9/cyclin T1
CHEMBL2111389
IC50 7.7 7.7 20.0 1
Cyclin-dependent kinase 13/Cyclin-K
CHEMBL4296067
IC50 7.53 7.53 29.3 1
CDK12/Cyclin K
CHEMBL4106169
IC50 7.13 7.13 74.4 1
BT-474
CHEMBL614529
IC50 6.31 6.31 490.0 1
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 6.03 6.03 932.0 1
CDK7/Cyclin H/MNAT1
CHEMBL3038473
IC50 5.92 5.92 1200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31477350 10.1016/j.bmcl.2019.126637 Cyclin-dependent kinase 2/cyclin E1 1
31477350 10.1016/j.bmcl.2019.126637 CDK9/cyclin T1 1
31477350 10.1016/j.bmcl.2019.126637 CDK7/Cyclin H/MNAT1 1
36827953 10.1016/j.ejmech.2023.115199 CDK12/Cyclin K 1
36827953 10.1016/j.ejmech.2023.115199 Cyclin-dependent kinase 13/Cyclin-K 1
36827953 10.1016/j.ejmech.2023.115199 BT-474 1

Data from ChEMBL 36 via Core Engine