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Compound Detail

CHEMBL4167139

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CC(C)(C)/C=C(/C#N)C(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1

Basic Information

ChEMBL ID CHEMBL4167139
Phase Preclinical
Structure Type MOL
InChI Key BRHJRWOQJXUVRF-CSMMYAOASA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

521.6
MW (Da)
5.53
ALogP
8
HBA
1
HBD
123.0
PSA (Ų)
0.27
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H31N7O2
MW 521.63
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.91

Activity Summary

IC50 1 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 8.4 8.4 4.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase BTK IC50 = 4.0 nM 8.4 Inhibition of BTK (unknown origin) 29631132

Literature References

PubMed DOI Target Context # Activities
29631132 10.1016/j.ejmech.2018.03.062 Tyrosine-protein kinase BTK 2
29631132 10.1016/j.ejmech.2018.03.062 Tyrosine-protein kinase JAK3 1

Data from ChEMBL 36 via Core Engine