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Compound Detail

CHEMBL2178263

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COCC(O)Cn1cc(NC(=O)c2cnn3cccnc23)c(-c2cccc(Cl)c2)n1

Basic Information

ChEMBL ID CHEMBL2178263
Phase Preclinical
Structure Type MOL
InChI Key HBFIQYJFDZYJOK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
4
Publications
0
Known Names

Molecular Properties

426.9
MW (Da)
2.51
ALogP
8
HBA
2
HBD
106.6
PSA (Ų)
0.47
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19ClN6O3
MW 426.86
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -2.13

Activity Summary

Ki 1 meas. best 7.78

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
Ki 7.78 7.78 16.7 1

Pharmacokinetic Data

Parameter Value Units Species
CL 32.0 mL.min-1.kg-1 Rattus norvegicus
CL 15.0 mL.min-1.kg-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase JAK2 Ki = 16.7 nM 7.78 Inhibition of purified JAK2 incubated for 30 mins 23061660

Literature References

PubMed DOI Target Context # Activities
23061660 10.1021/jm3012239 Unchecked 3
23061660 10.1021/jm3012239 Liver microsomes 2
23061660 10.1021/jm3012239 No relevant target 1
23061660 10.1021/jm3012239 Tyrosine-protein kinase JAK2 1

Data from ChEMBL 36 via Core Engine