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Compound Detail

CHEMBL4462032

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COc1ncc(-c2ccc3ncc(C(=O)NCc4cn(CCN5CCCC5)nn4)n3c2)cc1NS(=O)(=O)c1ccc(F)cc1F

Basic Information

ChEMBL ID CHEMBL4462032
Phase Preclinical
Structure Type MOL
InChI Key CCLGICLXKOTGBL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

637.7
MW (Da)
3.10
ALogP
11
HBA
2
HBD
148.6
PSA (Ų)
0.22
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29F2N9O4S
MW 637.67
Aromatic Rings 5
Heavy Atoms 45
NP-Likeness -2.20

Activity Summary

IC50 1 meas. best 5.45

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HCT-116
CHEMBL394
IC50 5.45 5.45 3540.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HCT-116 IC50 = 3540.0 nM 5.45 Cytotoxicity against human HCT116 cells harboring PIK3CA mutant assessed as redu... 32069401

Literature References

PubMed DOI Target Context # Activities
32069401 10.1021/acs.jmedchem.9b01736 HCT-116 1
32069401 10.1021/acs.jmedchem.9b01736 PI3-kinase p110-alpha/p85-alpha 1

Data from ChEMBL 36 via Core Engine