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Compound Detail

CHEMBL5629976

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C[N+]1([O-])CC[C@H](c2c(O)cc(O)c3c(=O)cc(/C=C/c4c(F)cccc4Cl)oc23)[C@H](O)C1

Basic Information

ChEMBL ID CHEMBL5629976
Phase Preclinical
Structure Type MOL
InChI Key RFGHAXHFSLZFPH-YQGNQTSOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

461.9
MW (Da)
3.96
ALogP
6
HBA
3
HBD
114.0
PSA (Ų)
0.40
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H21ClFNO6
MW 461.87
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness 0.82

Activity Summary

IC50 2 meas. best 5.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK9/cyclin T1
CHEMBL2111389
IC50 5.84 5.84 1430.0 1
Cyclin-dependent kinase 7/ cyclin H
CHEMBL2111288
IC50 5.29 5.29 5140.0 1

Activity Data Samples

Top measurements by pChEMBL value

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