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Compound Detail

CHEMBL4162057

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Cc1c(NC(=O)c2cc3c(s2)CCCC3)cccc1-c1cn(C)c(=O)c(Nc2ccc(C3C(=O)N(C)CCN3C)cc2)n1

Basic Information

ChEMBL ID CHEMBL4162057
Phase Preclinical
Structure Type MOL
InChI Key CDOOFZZILLRUQH-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

596.8
MW (Da)
5.14
ALogP
8
HBA
2
HBD
99.6
PSA (Ų)
0.32
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H36N6O3S
MW 596.76
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -1.38

Activity Summary

IC50 2 meas. best 8.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 8.23 8.23 5.9 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase BTK IC50 = 5.9 nM 8.23 Inhibition of BTK (unknown origin) 29631132
Tyrosine-protein kinase BTK IC50 = 5.9 nM 8.23 Reversible inhibition of human BTK 33773287

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
29631132 10.1016/j.ejmech.2018.03.062 Tyrosine-protein kinase BTK 1
33773287 10.1016/j.ejmech.2021.113356 Tyrosine-protein kinase BTK 1

Data from ChEMBL 36 via Core Engine