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Compound Detail

CHEMBL5269752

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COCC(=O)N1CCN2c3cc4c(N[C@H](C)c5cccc(C(F)F)c5F)nc(C)nc4cc3OC[C@H]2C1

Basic Information

ChEMBL ID CHEMBL5269752
Phase Preclinical
Structure Type MOL
InChI Key FKGUWCQKPBFTKO-GDBMZVCRSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

515.5
MW (Da)
4.24
ALogP
7
HBA
1
HBD
79.8
PSA (Ų)
0.53
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H28F3N5O3
MW 515.54
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.42

Activity Summary

IC50 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.0 8.0 10.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 860.0 ng.hr.mL-1 Mus musculus
Cmax 349.15 nM Mus musculus
MRT 3.43 hr Mus musculus
T1/2 5.86 hr Mus musculus
Tmax 0.83 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 10.0 nM 8.0 Inhibition of SOS1/KRAS G13D mutant protein-protein interaction in human DLD-1 c... 36384290

Literature References

PubMed DOI Target Context # Activities
36384290 10.1021/acs.jmedchem.2c01517 ADMET 6
36384290 10.1021/acs.jmedchem.2c01517 Unchecked 1

Data from ChEMBL 36 via Core Engine