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Compound Detail

CHEMBL5275185

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Cc1nc(N[C@H](C)c2cccc(C(F)F)c2F)c2cc3c(cc2n1)OC[C@H]1CN(C(=O)[C@@H]2C[C@H]2F)CCN31

Basic Information

ChEMBL ID CHEMBL5275185
Phase Preclinical
Structure Type MOL
InChI Key DHLBOJSMNOYRRN-GHIPVUKMSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
3
Publications
0
Known Names

Molecular Properties

529.5
MW (Da)
4.96
ALogP
6
HBA
1
HBD
70.6
PSA (Ų)
0.47
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27F4N5O2
MW 529.54
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.19

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.22 8.22 6.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 4010.0 ng.hr.mL-1 Mus musculus
Cmax 1229.37 nM Mus musculus
MRT 4.08 hr Mus musculus
T1/2 6.67 hr Mus musculus
Tmax 5.67 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 6.0 nM 8.22 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