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Compound Detail

CHEMBL5207401

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C=CC(=O)N(C)CCOc1cnccc1-c1ccc(CN2CCN(CC)CC2=O)c(C)c1

Basic Information

ChEMBL ID CHEMBL5207401
Phase Preclinical
Structure Type MOL
InChI Key JMIOWJADTBYGFC-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

436.6
MW (Da)
2.74
ALogP
5
HBA
0
HBD
66.0
PSA (Ų)
0.57
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H32N4O3
MW 436.56
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.05

Activity Summary

IC50 2 meas. best 7.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 7.5 7.5 32.0 1
Unchecked
CHEMBL612545
IC50 5.36 5.36 4410.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 113.0 mL.min-1.kg-1 Homo sapiens
CL 591.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35041943 10.1016/j.bmcl.2022.128549 Tyrosine-protein kinase BTK 2
35041943 10.1016/j.bmcl.2022.128549 ADMET 2
35041943 10.1016/j.bmcl.2022.128549 Unchecked 1

Data from ChEMBL 36 via Core Engine