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Compound Detail

CHEMBL4084955

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c1cc(-c2c[nH]c3cnccc23)ccn1

Basic Information

ChEMBL ID CHEMBL4084955
Phase Preclinical
Structure Type MOL
InChI Key KURWIPZCULOEEY-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

195.2
MW (Da)
2.62
ALogP
2
HBA
1
HBD
41.6
PSA (Ų)
0.65
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 C12H9N3
MW 195.22
Aromatic Rings 3
Heavy Atoms 15
NP-Likeness -0.26

Activity Summary

IC50 2 meas. best 9.0
EC50 1 meas. best 5.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
IC50 9.0 9.0 1.0 1
Nuclear factor of activated T-cells, cytoplasmic 1
CHEMBL3876
EC50 5.53 5.53 2980.0 1
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 5.04 5.04 9230.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28408219 10.1016/j.bmcl.2017.03.037 Ribosomal protein S6 kinase alpha-3 4
28408219 10.1016/j.bmcl.2017.03.037 Unchecked 4
28408219 10.1016/j.bmcl.2017.03.037 Serine/threonine-protein kinase MARK2 4
28408219 10.1016/j.bmcl.2017.03.037 Dual specificity mitogen-activated protein kinase kinase 1 3
28408219 10.1016/j.bmcl.2017.03.037 5'-AMP-activated protein kinase catalytic subunit alpha-2 3
28408219 10.1016/j.bmcl.2017.03.037 5'-AMP-activated protein kinase catalytic subunit alpha-1 3
28408219 10.1016/j.bmcl.2017.03.037 MAP/microtubule affinity-regulating kinase 4 3
28408219 10.1016/j.bmcl.2017.03.037 Tyrosine-protein kinase JAK1 3
28408219 10.1016/j.bmcl.2017.03.037 Serine/threonine-protein kinase WNK2 3
28408219 10.1016/j.bmcl.2017.03.037 Serine/threonine-protein kinase WNK1 3
28408219 10.1016/j.bmcl.2017.03.037 Ribosomal protein S6 kinase alpha-1 3
28408219 10.1016/j.bmcl.2017.03.037 MAP/microtubule affinity-regulating kinase 3 3
28408219 10.1016/j.bmcl.2017.03.037 Aurora kinase A 3
28408219 10.1016/j.bmcl.2017.03.037 Dual specificity mitogen-activated protein kinase kinase 2 3
28408219 10.1016/j.bmcl.2017.03.037 Tyrosine-protein kinase Fer 2
28408219 10.1016/j.bmcl.2017.03.037 Tyrosine-protein kinase ABL1 2
28408219 10.1016/j.bmcl.2017.03.037 STE20-like serine/threonine-protein kinase 2
28408219 10.1016/j.bmcl.2017.03.037 Tudor domain-containing protein 7 2
28408219 10.1016/j.bmcl.2017.03.037 Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma 2
28408219 10.1016/j.bmcl.2017.03.037 SRSF protein kinase 1 2

Data from ChEMBL 36 via Core Engine