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Compound Detail

CHEMBL313405

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N#Cc1ccc(Nc2nc(N)nc(Cc3c(Cl)ccc4[nH]ccc34)n2)cc1

Basic Information

ChEMBL ID CHEMBL313405
Phase Preclinical
Structure Type MOL
InChI Key SOKOHDQTKSROQZ-UHFFFAOYSA-N
1
Targets
14
Activities
2
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

375.8
MW (Da)
3.79
ALogP
6
HBA
3
HBD
116.3
PSA (Ų)
0.50
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C19H14ClN7
MW 375.82
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.59

Activity Summary

EC50 7 meas. best 8.52
IC50 7 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 8.52 7.1486 3.0 7
Human immunodeficiency virus 1
CHEMBL378
IC50 8.52 7.1486 3.0 7

Pharmacokinetic Data

Parameter Value Units Species
AUC 67500.0 ng.hr.mL-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus 1 EC50 = 3.0 nM 8.52 Potency evaluated against wild type HIV-1 strain IIIB 15115397
Human immunodeficiency virus 1 EC50 = 3.0 nM 8.52 Potency evaluated against NNRTI-Resistant HIV-1 strain Gly190Ala 15115397
Human immunodeficiency virus 1 IC50 = 3.0 nM 8.52 Antiviral activity against wild type HIV1 IIIB assessed as viral growth inhibiti... 35981459
Human immunodeficiency virus 1 IC50 = 3.0 nM 8.52 Antiviral activity against NNRTI resistant HIV1 harboring Gly190Ala mutant infec... 35981459
Human immunodeficiency virus 1 EC50 = 63.0 nM 7.2 Potency evaluated against NNRTI-Resistant HIV-1 strain Lys103Asn 15115397
Human immunodeficiency virus 1 EC50 = 63.0 nM 7.2 Potency evaluated against NNRTI-Resistant HIV-1 strain Val106Ala 15115397
Human immunodeficiency virus 1 IC50 = 63.0 nM 7.2 Antiviral activity against NNRTI resistant HIV1 harboring Lys103Asn mutant infec... 35981459
Human immunodeficiency virus 1 IC50 = 63.0 nM 7.2 Antiviral activity against NNRTI resistant HIV1 harboring Val106Ala mutant infec... 35981459
Human immunodeficiency virus 1 EC50 = 250.0 nM 6.6 Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr181Cys 15115397
Human immunodeficiency virus 1 IC50 = 250.0 nM 6.6 Antiviral activity against NNRTI resistant HIV1 harboring Tyr181Cys mutant infec... 35981459
Human immunodeficiency virus 1 EC50 = 1000.0 nM 6.0 Potency evaluated against NNRTI-Resistant HIV-1 strain Leu100Ile 15115397
Human immunodeficiency virus 1 EC50 = 1000.0 nM 6.0 Potency evaluated against NNRTI-Resistant HIV-1 strain Tyr188Leu 15115397
Human immunodeficiency virus 1 IC50 = 1000.0 nM 6.0 Antiviral activity against NNRTI resistant HIV1 harboring Leu100IIe mutant infec... 35981459
Human immunodeficiency virus 1 IC50 = 1000.0 nM 6.0 Antiviral activity against NNRTI resistant HIV1 harboring Tyr188Leu mutant infec... 35981459

Literature References

PubMed DOI Target Context # Activities
15115397 10.1021/jm030558s Human immunodeficiency virus 1 7
35981459 10.1016/j.ejmech.2022.114645 Human immunodeficiency virus 1 7
15771441 10.1021/jm049439i ADMET 1
15771441 10.1021/jm049439i No relevant target 1

Data from ChEMBL 36 via Core Engine