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Compound Detail

CHEMBL4756388

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COc1cc2c(cc1OC)/C(=C/COCc1c(-c3ccc(F)cc3)nc(N(C)S(C)(=O)=O)nc1C(C)C)OC2=O

Basic Information

ChEMBL ID CHEMBL4756388
Phase Preclinical
Structure Type MOL
InChI Key QPDRWVMTBQDYLF-JJFYIABZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

571.6
MW (Da)
4.55
ALogP
9
HBA
0
HBD
117.2
PSA (Ų)
0.26
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30FN3O7S
MW 571.63
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.28

Activity Summary

IC50 1 meas. best 5.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 5.43 5.43 3700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
RAC-alpha serine/threonine-protein kinase IC50 = 3700.0 nM 5.43 Inhibition of Akt-1 (unknown origin) 32599323

Literature References

PubMed DOI Target Context # Activities
32599323 10.1016/j.ejmech.2020.112335 ADMET 5
32599323 10.1016/j.ejmech.2020.112335 Unchecked 4
32599323 10.1016/j.ejmech.2020.112335 RAC-alpha serine/threonine-protein kinase 2
32599323 10.1016/j.ejmech.2020.112335 HCT-116 1
32599323 10.1016/j.ejmech.2020.112335 HepG2 1
32599323 10.1016/j.ejmech.2020.112335 PA-1 1
32599323 10.1016/j.ejmech.2020.112335 PANC-1 1
32599323 10.1016/j.ejmech.2020.112335 RAC-beta serine/threonine-protein kinase 1

Data from ChEMBL 36 via Core Engine