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Compound Detail

CHEMBL5597425

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CCC(=O)Nc1cccc(Cn2cnc3c(F)c(Nc4ccc(C5CC5)cc4F)c(C(=O)NOCCO)cc32)c1

Basic Information

ChEMBL ID CHEMBL5597425
Phase Preclinical
Structure Type MOL
InChI Key WGJIDJNVIXCIPN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

549.6
MW (Da)
4.99
ALogP
7
HBA
4
HBD
117.5
PSA (Ų)
0.15
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29F2N5O4
MW 549.58
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.35

Activity Summary

IC50 1 meas. best 6.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MIA PaCa-2
CHEMBL614725
IC50 6.01 6.01 985.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MIA PaCa-2 IC50 = 985.0 nM 6.01 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