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Compound Detail

CHEMBL1825043

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c1ccc(Cn2cc(-c3ccccc3)nn2)cc1

Basic Information

ChEMBL ID CHEMBL1825043
Phase Preclinical
Structure Type MOL
InChI Key GANAQXGHGKBVKP-UHFFFAOYSA-N
4
Targets
8
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

235.3
MW (Da)
2.99
ALogP
3
HBA
0
HBD
30.7
PSA (Ų)
0.70
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 C15H13N3
MW 235.29
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -1.66

Activity Summary

IC50 8 meas. best 5.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
IC50 5.01 5.01 9770.0 1
Leishmania donovani
CHEMBL367
IC50 4.07 4.07 85000.0 1
B16-F10
CHEMBL612656
IC50 4.02 4.02 96100.0 1
P388
CHEMBL389
IC50 4.0 4.0 99100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22981330 10.1016/j.bmcl.2012.08.067 Sodium channel protein type 8 subunit alpha 2
21703734 10.1016/j.ejmech.2011.05.074 Aromatase 1
21944473 10.1016/j.ejmech.2011.09.013 Enoyl-[acyl-carrier-protein] reductase [NADH] 1
21944473 10.1016/j.ejmech.2011.09.013 Mycobacterium tuberculosis 1
22616902 10.1021/jm300260v Indoleamine 2,3-dioxygenase 1 1
29198863 10.1016/j.bmcl.2017.11.038 B16-F10 1
29198863 10.1016/j.bmcl.2017.11.038 P388 1
29198863 10.1016/j.bmcl.2017.11.038 HL-60 1
29198863 10.1016/j.bmcl.2017.11.038 KB 1
29198863 10.1016/j.bmcl.2017.11.038 HT-1080 1
29198863 10.1016/j.bmcl.2017.11.038 MCF7 1
29198863 10.1016/j.bmcl.2017.11.038 DLD-1 1
29198863 10.1016/j.bmcl.2017.11.038 NUGC-3 1
29198863 10.1016/j.bmcl.2017.11.038 Unchecked 1
36760749 10.1039/d2md00324d Leishmania donovani 1

Data from ChEMBL 36 via Core Engine