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Compound Detail

CHEMBL4164030

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

Basic Information

ChEMBL ID CHEMBL4164030
Phase Preclinical
Structure Type MOL
InChI Key CYYRPFWAMVGRGT-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

522.6
MW (Da)
4.04
ALogP
6
HBA
2
HBD
87.4
PSA (Ų)
0.49
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29F3N6O
MW 522.58
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -1.57

Activity Summary

IC50 3 meas. best 8.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epithelial discoidin domain-containing receptor 1
CHEMBL5319
IC50 8.41 8.41 3.9 1
Tyrosine-protein kinase ABL1
CHEMBL1862
IC50 7.68 7.68 21.0 1
Discoidin domain-containing receptor 2
CHEMBL5122
IC50 7.34 7.34 45.3 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