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Compound Detail

CHEMBL5208570

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Cc1cc(-c2ccnc(Nc3cnn(C4CN(C)C4)c3)n2)ccc1CN1CCN(CC(C)(C)C)CC1=O

Basic Information

ChEMBL ID CHEMBL5208570
Phase Preclinical
Structure Type MOL
InChI Key WFNHWZJHEKXXQV-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

502.7
MW (Da)
3.57
ALogP
8
HBA
1
HBD
82.4
PSA (Ų)
0.53
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H38N8O
MW 502.67
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.43

Activity Summary

IC50 2 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 8.15 6.865 7.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase BTK IC50 = 7.0 nM 8.15 Inhibition of BTK (unknown origin) 35041943
Tyrosine-protein kinase BTK IC50 = 2650.0 nM 5.58 Inhibition of pBTK in human whole blood 35041943

Literature References

PubMed DOI Target Context # Activities
35041943 10.1016/j.bmcl.2022.128549 Tyrosine-protein kinase BTK 2

Data from ChEMBL 36 via Core Engine