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Compound Detail

CHEMBL5573404

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CCn1cnc2c(NCc3ccc(-n4cccn4)nc3)nc(N3CCCC[C@H]3CCO)nc21

Basic Information

ChEMBL ID CHEMBL5573404
Phase Preclinical
Structure Type MOL
InChI Key ADBAHGUKYCECGO-SFHVURJKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

447.6
MW (Da)
2.78
ALogP
10
HBA
2
HBD
109.8
PSA (Ų)
0.42
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H29N9O
MW 447.55
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.77

Activity Summary

IC50 1 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK12/Cyclin K
CHEMBL4106169
IC50 8.52 8.52 3.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK12/Cyclin K IC50 = 3.0 nM 8.52 Inhibition of recombinant human CDK12/Cyclin K using RNA Pol II-CTD as substrate... 38061230

Literature References

PubMed DOI Target Context # Activities
38061230 10.1016/j.ejmech.2023.116014 CDK12/Cyclin K 1
38061230 10.1016/j.ejmech.2023.116014 SK-BR-3 1
38061230 10.1016/j.ejmech.2023.116014 HCC1954 1

Data from ChEMBL 36 via Core Engine