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Compound Detail

CHEMBL5271862

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Cc1nc(N[C@H](C)c2cccc(C(F)F)c2F)c2cc3c(cc2n1)OC[C@H]1CN(C(=O)[C@@H]2CCOC2)CCN31

Basic Information

ChEMBL ID CHEMBL5271862
Phase Preclinical
Structure Type MOL
InChI Key HGHGNXYWUVTGMS-KBAYOESNSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

541.6
MW (Da)
4.63
ALogP
7
HBA
1
HBD
79.8
PSA (Ų)
0.50
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30F3N5O3
MW 541.57
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -1.22

Activity Summary

IC50 1 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.68 7.68 21.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 780.0 ng.hr.mL-1 Mus musculus
Cmax 86.78 nM Mus musculus
MRT 9.65 hr Mus musculus
T1/2 18.0 hr Mus musculus
Tmax 8.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 21.0 nM 7.68 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