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Compound Detail

CHEMBL5594350

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CP(C)(=O)c1cc(F)cc2c(-c3nc(N[C@H]4CCCNC4)nc4ccsc34)c[nH]c12

Basic Information

ChEMBL ID CHEMBL5594350
Phase Preclinical
Structure Type MOL
InChI Key ROBBURZERULYQU-ZDUSSCGKSA-N
2
Targets
2
Activities
2
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

443.5
MW (Da)
4.39
ALogP
6
HBA
3
HBD
82.7
PSA (Ų)
0.41
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23FN5OPS
MW 443.49
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.08

Activity Summary

EC50 1 meas. best 6.92
IC50 1 meas. best 8.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK7/Cyclin H/MNAT1
CHEMBL3038473
IC50 8.06 8.06 8.7 1
MDA-MB-453
CHEMBL614334
EC50 6.92 6.92 120.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.0 hr Homo sapiens
T1/2 0.25 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38000213 10.1016/j.ejmech.2023.115955 ADMET 2
38000213 10.1016/j.ejmech.2023.115955 CDK7/Cyclin H/MNAT1 1
38000213 10.1016/j.ejmech.2023.115955 MDA-MB-453 1

Data from ChEMBL 36 via Core Engine