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Compound Detail

CHEMBL5598403

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CNS(=O)(=O)Nc1cc(Cn2cnc3c(F)c(Nc4ccc(C5CC5)cc4F)c(C(=O)NOCCO)cc32)ccc1F

Basic Information

ChEMBL ID CHEMBL5598403
Phase Preclinical
Structure Type MOL
InChI Key GJIQWSHTRPAARL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

604.6
MW (Da)
3.65
ALogP
8
HBA
5
HBD
146.6
PSA (Ų)
0.12
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27F3N6O5S
MW 604.61
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -1.23

Activity Summary

IC50 1 meas. best 6.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MIA PaCa-2
CHEMBL614725
IC50 6.21 6.21 611.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MIA PaCa-2 IC50 = 611.0 nM 6.21 Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mu... 39166848

Literature References

PubMed DOI Target Context # Activities
39166848 10.1021/acs.jmedchem.4c00860 MIA PaCa-2 2
39166848 10.1021/acs.jmedchem.4c00860 HCT-116 2
39166848 10.1021/acs.jmedchem.4c00860 Dual specificity mitogen-activated protein kinase kinase 1 1
39166848 10.1021/acs.jmedchem.4c00860 Serine/threonine-protein kinase B-raf 1

Data from ChEMBL 36 via Core Engine