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Compound Detail

CHEMBL4075640

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O=C(Nc1nc(-c2ccccc2)cn2cc(-c3ccccc3)nc12)c1ccccc1

Basic Information

ChEMBL ID CHEMBL4075640
Phase Preclinical
Structure Type MOL
InChI Key CEDLTEINBRKAJS-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

390.4
MW (Da)
5.32
ALogP
4
HBA
1
HBD
59.3
PSA (Ų)
0.45
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H18N4O
MW 390.45
Aromatic Rings 5
Heavy Atoms 30
NP-Likeness -1.08

Activity Summary

IC50 2 meas. best 6.63
Ki 1 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transmembrane domain-containing protein TMIGD3
CHEMBL3712907
Ki 7.09 7.09 82.0 1
Adenosine receptor A3
CHEMBL256
IC50 6.63 6.63 235.0 1
Transmembrane domain-containing protein TMIGD3
CHEMBL3712907
IC50 6.63 6.63 235.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27721147 10.1016/j.ejmech.2016.09.076 Transmembrane domain-containing protein TMIGD3 2
27721147 10.1016/j.ejmech.2016.09.076 Adenosine receptor A1 1
27721147 10.1016/j.ejmech.2016.09.076 Adenosine receptor A2a 1
27721147 10.1016/j.ejmech.2016.09.076 Adenosine receptor A2b 1
27721147 10.1016/j.ejmech.2016.09.076 Adenosine receptor A3 1
34695776 10.1016/j.ejmech.2021.113907 Adenosine receptor A3 1

Data from ChEMBL 36 via Core Engine