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Compound Detail

CHEMBL5274075

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Cc1nc(N[C@H](C)c2cccc(C(F)F)c2F)c2cc3c(cc2n1)OC[C@H]1CN(C(=O)NC2CC2)CCN31

Basic Information

ChEMBL ID CHEMBL5274075
Phase Preclinical
Structure Type MOL
InChI Key JCDHHDRIBUMCFN-RHSMWYFYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
3
Publications
0
Known Names

Molecular Properties

526.6
MW (Da)
4.94
ALogP
6
HBA
2
HBD
82.6
PSA (Ų)
0.49
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H29F3N6O2
MW 526.56
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.48

Activity Summary

IC50 1 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.1 8.1 8.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3490.0 ng.hr.mL-1 Mus musculus
Cmax 1057.81 nM Mus musculus
MRT 4.36 hr Mus musculus
T1/2 12.6 hr Mus musculus
Tmax 6.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 8.0 nM 8.1 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 8
36384290 10.1021/acs.jmedchem.2c01517 Unchecked 1
36384290 10.1021/acs.jmedchem.2c01517 MIA PaCa-2 1

Data from ChEMBL 36 via Core Engine