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Compound Detail

CHEMBL1086473

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CCCCc1nc2c(N)nc3ccccc3c2n1Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL1086473
Phase Preclinical
Structure Type MOL
InChI Key CQBDMXYZNLJUFT-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
1
PK Parameters
14
Publications
0
Known Names

Molecular Properties

330.4
MW (Da)
4.56
ALogP
4
HBA
1
HBD
56.7
PSA (Ų)
0.58
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 C21H22N4
MW 330.44
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.92

Activity Summary

EC50 3 meas. best 7.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Toll-like receptor 7
CHEMBL5936
EC50 7.23 6.8433 59.1 3

Pharmacokinetic Data

Parameter Value Units Species
CL 6.0 mL.min-1.g-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30850167 10.1016/j.bmcl.2019.02.029 Plasmodium berghei 32
30850167 10.1016/j.bmcl.2019.02.029 ADMET 7
34527180 10.1021/acsmedchemlett.1c00267 ADMET 5
23899291 10.1021/jm400694d Toll-like receptor 8 4
- 10.6019/CHEMBL3301361 ADMET 2
34527180 10.1021/acsmedchemlett.1c00267 Unchecked 2
20481492 10.1021/jm100358c Toll-like receptor 8 1
20481492 10.1021/jm100358c Blood 1
20481492 10.1021/jm100358c Toll-like receptor 7 1
- 10.6019/CHEMBL3301361 No relevant target 1
34527180 10.1021/acsmedchemlett.1c00267 TLR7 and TLR8 1
37163340 10.1021/acs.jmedchem.2c01655 Toll-like receptor 7 1
38741265 10.1021/acs.jmedchem.4c00464 Toll-like receptor 7 1
38741265 10.1021/acs.jmedchem.4c00464 Toll-like receptor 8 1

Data from ChEMBL 36 via Core Engine