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Compound Detail

CHEMBL2152307

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c1ncc(CN2CCC(n3cnc4cnc5[nH]ccc5c43)CC2)cn1

Basic Information

ChEMBL ID CHEMBL2152307
Phase Preclinical
Structure Type MOL
InChI Key YNEDMIROJZALTC-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

333.4
MW (Da)
2.54
ALogP
6
HBA
1
HBD
75.5
PSA (Ų)
0.62
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H19N7
MW 333.40
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -1.10

Activity Summary

EC50 1 meas. best 6.46
Ki 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK1
CHEMBL2835
Ki 8.7 8.7 2.0 1
Tyrosine-protein kinase JAK1
CHEMBL2835
EC50 6.46 6.46 350.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 4.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22591402 10.1021/jm300438j Tyrosine-protein kinase JAK1 2
22591402 10.1021/jm300438j Unchecked 2
22591402 10.1021/jm300438j Liver microsomes 1

Data from ChEMBL 36 via Core Engine