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Compound Detail

CHEMBL380071

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c1ccc2c(-c3ccncc3)c[nH]c2c1

Basic Information

ChEMBL ID CHEMBL380071
Phase Preclinical
Structure Type MOL
InChI Key LLJRXVHJOJRCSM-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

194.2
MW (Da)
3.23
ALogP
1
HBA
1
HBD
28.7
PSA (Ų)
0.63
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H10N2
MW 194.24
Aromatic Rings 3
Heavy Atoms 15
NP-Likeness -0.37

Activity Summary

IC50 3 meas. best 5.94

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inosine-5'-monophosphate dehydrogenase 2
CHEMBL2002
IC50 5.94 5.94 1150.0 2
PBMC
CHEMBL613107
IC50 4.55 4.55 28000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Inosine-5'-monophosphate dehydrogenase 2 IC50 = 1150.0 nM 5.94 Inhibition of IMPDH2 16483769
Inosine-5'-monophosphate dehydrogenase 2 IC50 = 1150.0 nM 5.94 Inhibition of IMPDH2 16483773
PBMC IC50 = 28000.0 nM 4.55 Antiproliferative activity against PBMC 16483773

Literature References

PubMed DOI Target Context # Activities
23398362 10.1042/bj20121418 Insulin-like growth factor 1 receptor 4
23398362 10.1042/bj20121418 Tyrosine-protein kinase HCK 4
23398362 10.1042/bj20121418 Serine/threonine-protein kinase mTOR 4
23398362 10.1042/bj20121418 Tyrosine-protein kinase Lck 4
23398362 10.1042/bj20121418 Protein kinase C beta type 4
23398362 10.1042/bj20121418 cGMP-dependent protein kinase 1 4
23398362 10.1042/bj20121418 Cyclin-dependent kinase 5/CDK5 activator 1 4
23398362 10.1042/bj20121418 Insulin receptor 4
23398362 10.1042/bj20121418 SRSF protein kinase 3 2
23398362 10.1042/bj20121418 Serine/threonine-protein kinase MARK1 2
23398362 10.1042/bj20121418 3-phosphoinositide-dependent protein kinase 1 2
23398362 10.1042/bj20121418 Aurora kinase A 2
23398362 10.1042/bj20121418 Cyclin-dependent kinase 2/cyclin A 2
23398362 10.1042/bj20121418 Cyclin-dependent kinase 2/cyclin E 2
23398362 10.1042/bj20121418 Casein kinase I isoform gamma-3 2
23398362 10.1042/bj20121418 Casein kinase I isoform delta 2
23398362 10.1042/bj20121418 Death-associated protein kinase 1 2
16483773 10.1016/j.bmcl.2006.01.090 Caco-2 2
23398362 10.1042/bj20121418 Fibroblast growth factor receptor 3 2
23398362 10.1042/bj20121418 Tyrosine-protein kinase Fyn 2

Data from ChEMBL 36 via Core Engine