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Compound Detail

CHEMBL3103988

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N#Cc1cccc(-c2nc(-c3cccnc3)no2)c1

Basic Information

ChEMBL ID CHEMBL3103988
Phase Preclinical
Structure Type MOL
InChI Key HGFXDSQLRSWUBO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

248.2
MW (Da)
2.67
ALogP
5
HBA
0
HBD
75.6
PSA (Ų)
0.70
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H8N4O
MW 248.25
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -2.22

Activity Summary

EC50 2 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nicotinic acetylcholine receptor alpha4/beta2/alpha5
CHEMBL3038461
EC50 6.1 6.1 790.0 1
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907589
EC50 6.0 6.0 990.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5303304 Fibroblast 8
- 10.6019/CHEMBL5303304 HEK-293T 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
24365158 10.1016/j.bmcl.2013.11.049 Nicotinic acetylcholine receptor alpha4/beta2/alpha5 3
- 10.6019/CHEMBL5303304 U2OS 3
24365158 10.1016/j.bmcl.2013.11.049 Neuronal acetylcholine receptor; alpha4/beta2 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
24365158 10.1016/j.bmcl.2013.11.049 Neuronal acetylcholine receptor; alpha3/beta4 1
24365158 10.1016/j.bmcl.2013.11.049 Nicotinic acetylcholine receptor alpha3/beta4/alpha5 1
24365158 10.1016/j.bmcl.2013.11.049 Neuronal acetylcholine receptor; alpha3/beta2 1
24365158 10.1016/j.bmcl.2013.11.049 Nicotinic acetylcholine receptor alpha3/beta2/alpha5 1
- 10.6019/CHEMBL5665443 Methyl-CpG-binding domain protein 4 1
- 10.6019/CHEMBL5665443 DNA-3-methyladenine glycosylase 1
- 10.6019/CHEMBL5665443 Adenine DNA glycosylase 1
- 10.6019/CHEMBL5665443 Endonuclease 8-like 1 1
- 10.6019/CHEMBL5665443 Endonuclease 8-like 2 1
- 10.6019/CHEMBL5665443 Endonuclease III-like protein 1 1
- 10.6019/CHEMBL5665443 N-glycosylase/DNA lyase 1

Data from ChEMBL 36 via Core Engine