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Compound Detail

CHEMBL400403

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Cc1cc(-c2cc(O)ccc2Cl)cc2nnc(Nc3ccc(C(=O)NCCN4CCCC4)cc3)nc12

Basic Information

ChEMBL ID CHEMBL400403
Phase Preclinical
Structure Type MOL
InChI Key UQNMVTOJPFMVNB-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

503.0
MW (Da)
4.93
ALogP
7
HBA
3
HBD
103.3
PSA (Ų)
0.33
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H27ClN6O2
MW 503.01
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.26

Activity Summary

Ki 2 meas. best 8.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ABL1
CHEMBL1862
Ki 8.59 7.955 2.6 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase ABL1 Ki = 2.6 nM 8.59 Inhibition of Abl 17827012
Tyrosine-protein kinase ABL1 Ki = 48.0 nM 7.32 Inhibition of Abl-T315I mutant 17827012

Literature References

PubMed DOI Target Context # Activities
17827012 10.1016/j.bmcl.2007.08.043 Tyrosine-protein kinase ABL1 2

Data from ChEMBL 36 via Core Engine