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Compound Detail

CHEMBL5630758

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CCOc1cc(O)c2c(=O)cc(/C=C/c3c(F)cccc3Cl)oc2c1[C@H]1CC[N+](C)([O-])C[C@H]1O

Basic Information

ChEMBL ID CHEMBL5630758
Phase Preclinical
Structure Type MOL
InChI Key GTQVSRPKTWDJFA-DRBYBZGTSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

489.9
MW (Da)
4.65
ALogP
6
HBA
2
HBD
103.0
PSA (Ų)
0.40
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H25ClFNO6
MW 489.93
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness 0.65

Activity Summary

IC50 1 meas. best 6.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK9/cyclin T1
CHEMBL2111389
IC50 6.35 6.35 450.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK9/cyclin T1 IC50 = 450.0 nM 6.35 Inhibition of CDK9/cyclin T1 (unknown origin) by ADP-Glo assay 37302342

Literature References

PubMed DOI Target Context # Activities
37302342 10.1016/j.ejmech.2023.115533 Cyclin-dependent kinase 7/ cyclin H 2
37302342 10.1016/j.ejmech.2023.115533 CDK9/Cyclin K 2
37302342 10.1016/j.ejmech.2023.115533 HCT-116 2
37302342 10.1016/j.ejmech.2023.115533 MIA PaCa-2 2
37302342 10.1016/j.ejmech.2023.115533 HEK293 2
37302342 10.1016/j.ejmech.2023.115533 CDK9/cyclin T1 1

Data from ChEMBL 36 via Core Engine