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Compound Detail

CHEMBL4111121

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Nc1nccn2c([C@@H]3CC[C@H]4CN(CC(=O)O)CC(=O)N4C3)nc(-c3ccc(C(=O)Nc4cc(C(F)(F)F)ccn4)cc3)c12

Basic Information

ChEMBL ID CHEMBL4111121
Phase Preclinical
Structure Type MOL
InChI Key PWFPFIZORJMGLA-QUCCMNQESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

608.6
MW (Da)
3.12
ALogP
9
HBA
3
HBD
159.1
PSA (Ų)
0.30
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H27F3N8O4
MW 608.58
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -1.14

Activity Summary

IC50 1 meas. best 9.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 9.66 9.66 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase BTK IC50 = 0.22 nM 9.66 LANCE (Lanthanide Chelate Excite) TR-FRET (Time-resolved fluorescence resonance ... -

Data from ChEMBL 36 via Core Engine