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Compound Detail

CHEMBL4174682

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CCc1ccc(C(=O)Nc2cc(CN3CCN(C)CC3)cc(C(F)(F)F)c2)cc1C#Cc1cnc(NC)nc1

Basic Information

ChEMBL ID CHEMBL4174682
Phase Preclinical
Structure Type MOL
InChI Key UEHGHDJPDQDZPX-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

536.6
MW (Da)
4.50
ALogP
6
HBA
2
HBD
73.4
PSA (Ų)
0.45
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31F3N6O
MW 536.60
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -1.56

Activity Summary

IC50 3 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epithelial discoidin domain-containing receptor 1
CHEMBL5319
IC50 8.3 8.3 5.0 1
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 7.52 7.52 30.2 1
Discoidin domain-containing receptor 2
CHEMBL5122
IC50 7.08 7.08 83.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30075624 10.1021/acs.jmedchem.8b01045 Epithelial discoidin domain-containing receptor 1 1
30075624 10.1021/acs.jmedchem.8b01045 Tyrosine-protein kinase ABL1 1
30075624 10.1021/acs.jmedchem.8b01045 Discoidin domain-containing receptor 2 1

Data from ChEMBL 36 via Core Engine