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Compound Detail

CHEMBL3670081

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Cn1cc(-c2cccc(N3CCc4c(sc5c4CCCC5)C3=O)c2CO)cc(Nc2ccncn2)c1=O

Basic Information

ChEMBL ID CHEMBL3670081
Phase Preclinical
Structure Type MOL
InChI Key LRUSCQLECOYKHK-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

513.6
MW (Da)
4.22
ALogP
8
HBA
2
HBD
100.3
PSA (Ų)
0.41
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 C28H27N5O3S
MW 513.62
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.97

Activity Summary

IC50 3 meas. best 9.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 9.06 9.03 0.9 2
Tyrosine-protein kinase BTK
CHEMBL3259478
IC50 7.06 7.06 87.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.0 mL.min-1.kg-1 Rattus norvegicus
F 90.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28626519 10.1021/acsmedchemlett.7b00103 Tyrosine-protein kinase BTK 2
28626519 10.1021/acsmedchemlett.7b00103 Rattus norvegicus 2
28626519 10.1021/acsmedchemlett.7b00103 Plasma 1
28626519 10.1021/acsmedchemlett.7b00103 No relevant target 1

Data from ChEMBL 36 via Core Engine