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Compound Detail

CHEMBL3981886

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COc1ccc(C(=O)N2CCC(N3CC(CC#N)(n4cc(-c5ncnc6[nH]ccc56)cn4)C3)CC2)cc1C#N

Basic Information

ChEMBL ID CHEMBL3981886
Phase Preclinical
Structure Type MOL
InChI Key JHMOGMFDLJUAQS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
0
Publications
0
Known Names

Molecular Properties

521.6
MW (Da)
2.93
ALogP
9
HBA
1
HBD
139.8
PSA (Ų)
0.41
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 C28H27N9O2
MW 521.59
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.01

Activity Summary

IC50 1 meas. best 7.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
IC50 7.52 7.52 30.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase JAK2 IC50 = 30.0 nM 7.52 In vitro JAK Kinase Assay: The catalytic domains of human JAK1 (a.a. 837-1142), ... -

Data from ChEMBL 36 via Core Engine