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Compound Detail

CHEMBL1082399

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C=CCCc1nc2c(N)nc3ccccc3c2n1Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL1082399
Phase Preclinical
Structure Type MOL
InChI Key PJPBMTWYSAFQON-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

328.4
MW (Da)
4.33
ALogP
4
HBA
1
HBD
56.7
PSA (Ų)
0.55
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20N4
MW 328.42
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.66

Activity Summary

EC50 1 meas. best 6.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Toll-like receptor 7
CHEMBL5936
EC50 6.58 6.58 262.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Toll-like receptor 7 EC50 = 262.0 nM 6.58 Agonist activity at human TLR7 expressed in NF-kappaB-stimulated HEK293 cells as... 20481492

Literature References

PubMed DOI Target Context # Activities
20481492 10.1021/jm100358c Toll-like receptor 8 1
20481492 10.1021/jm100358c Toll-like receptor 7 1

Data from ChEMBL 36 via Core Engine