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Compound Detail

CHEMBL5277035

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Cc1nc(N[C@H](C)c2cccc(C(F)F)c2F)c2cc3c(cc2n1)OC[C@H]1CN(C(=O)C2CCO2)CCN31

Basic Information

ChEMBL ID CHEMBL5277035
Phase Preclinical
Structure Type MOL
InChI Key JLKUIBYUMFJLMH-IMRCFTKNSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

527.5
MW (Da)
4.39
ALogP
7
HBA
1
HBD
79.8
PSA (Ų)
0.53
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28F3N5O3
MW 527.55
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.25

Activity Summary

IC50 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.8 7.8 16.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 534.0 ng.hr.mL-1 Mus musculus
Cmax 184.06 nM Mus musculus
MRT 4.55 hr Mus musculus
T1/2 14.3 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 = 16.0 nM 7.8 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