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Compound Detail

CHEMBL205177

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N#Cc1ccc(C(c2ccc3[nH]ccc3c2)n2ccnc2)cc1

Basic Information

ChEMBL ID CHEMBL205177
Phase Preclinical
Structure Type MOL
InChI Key XASLSINSUIIGRS-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

298.4
MW (Da)
3.87
ALogP
3
HBA
1
HBD
57.4
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 C19H14N4
MW 298.35
Aromatic Rings 4
Heavy Atoms 23
NP-Likeness -1.18

Activity Summary

IC50 2 meas. best 7.71

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
IC50 7.71 7.71 19.3 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Aromatase IC50 = 19.3 nM 7.71 Inhibition of CYP19 16380254
Aromatase IC50 = 19.3 nM 7.71 Inhibition of aromatase in human placental microsomes 18640836

Literature References

PubMed DOI Target Context # Activities
16380254 10.1016/j.bmcl.2005.11.099 Aromatase 2
16380254 10.1016/j.bmcl.2005.11.099 Steroid 17-alpha-hydroxylase/17,20 lyase 1
18640836 10.1016/j.bmcl.2008.06.094 Aromatase 1

Data from ChEMBL 36 via Core Engine