Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL307297

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
N#Cc1ccc(Nc2nc(N)nc(Cc3c(Cl)cccc3Cl)n2)cc1

Basic Information

ChEMBL ID CHEMBL307297
Phase Preclinical
Structure Type MOL
InChI Key BYARTTHGWGIRGS-UHFFFAOYSA-N
3
Targets
35
Activities
2
Assay Types
1
PK Parameters
8
Publications
0
Known Names

Molecular Properties

371.2
MW (Da)
3.97
ALogP
6
HBA
2
HBD
100.5
PSA (Ų)
0.72
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H12Cl2N6
MW 371.23
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.78

Activity Summary

IC50 23 meas. best 9.0
EC50 12 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 9.0 7.4471 1.0 7
Human immunodeficiency virus 1
CHEMBL378
IC50 9.0 7.2794 1.0 18
Human immunodeficiency virus type 1 reverse transcriptase
CHEMBL247
IC50 8.22 7.044 6.0 5
MT4
CHEMBL388
EC50 8.22 7.044 6.0 5

Pharmacokinetic Data

Parameter Value Units Species
AUC 1500.0 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 = 1.0 nM 9.0 Potency evaluated against NNRTI-Resistant HIV-1 strain Gly190Ala 15115397
Human immunodeficiency virus 1 IC50 = 1.0 nM 9.0 Antiviral activity against NNRTI resistant HIV1 harboring Gly190Ala mutant infec... 35981459
Human immunodeficiency virus 1 EC50 = 2.0 nM 8.7 Potency evaluated against wild type HIV-1 strain IIIB 15115397
Human immunodeficiency virus 1 IC50 = 2.0 nM 8.7 Antiviral activity against wild type HIV1 IIIB assessed as viral growth inhibiti... 35981459
MT4 EC50 = 6.0 nM 8.22 Effective concentration of the compound to inhibit HIV-1 mutant LAI replication ... 15771411
Human immunodeficiency virus type 1 reverse transcriptase IC50 = 6.0 nM 8.22 Inhibition of HIV1 LAI reverse transcriptase infected in human MT4 cells assesse... 30223123
Human immunodeficiency virus 1 IC50 = 6.0 nM 8.22 Inhibitory activity against LAI strain of HIV-I in MT-4 cells 11527705
Human immunodeficiency virus 1 IC50 = 6.3 nM 8.2 Antiviral activity against NNRTI resistant HIV1 LAI infected in human MT4 cells ... 35981459
Human immunodeficiency virus 1 IC50 = 6.3 nM 8.2 Inhibitory activity against LAI strain of HIV-I in MT-4 cell was determined 11527704
Human immunodeficiency virus 1 EC50 = 26.0 nM 7.58 Potency evaluated against NNRTI-Resistant HIV-1 strain Val106Ala 15115397
Human immunodeficiency virus 1 IC50 = 26.0 nM 7.58 Antiviral activity against NNRTI resistant HIV1 harboring Val106Ala mutant infec... 35981459
MT4 EC50 = 40.0 nM 7.4 Effective concentration of the compound to inhibit HIV-1 mutant K103N replicatio... 15771411
Human immunodeficiency virus 1 IC50 = 40.0 nM 7.4 Inhibitory activity against 103N strain of HIV-I in MT-4 cell was determined 11527704
Human immunodeficiency virus 1 IC50 = 40.0 nM 7.4 Inhibitory activity against 103N strain of HIV-I in MT-4 cells 11527705
Human immunodeficiency virus type 1 reverse transcriptase IC50 = 40.0 nM 7.4 Inhibition of HIV1 reverse transcriptase K103N mutant infected in human MT4 cell... 30223123
Human immunodeficiency virus 1 IC50 = 40.0 nM 7.4 Antiviral activity against NNRTI resistant HIV1 harboring Lys103Asn mutant infec... 35981459
Human immunodeficiency virus 1 EC50 = 41.0 nM 7.39 Potency evaluated against NNRTI-Resistant HIV-1 strain Lys103Asn 15115397
Human immunodeficiency virus 1 IC50 = 200.0 nM 6.7 Antiviral activity against NNRTI resistant HIV1 harboring Tyr181Cys mutant infec... 35981459
Human immunodeficiency virus type 1 reverse transcriptase IC50 = 200.0 nM 6.7 Inhibition of HIV1 reverse transcriptase Y181C mutant infected in human MT4 cell... 30223123
Human immunodeficiency virus 1 IC50 = 200.0 nM 6.7 Inhibitory activity against 181C strain of HIV-I in MT-4 cells 11527705

Literature References

PubMed DOI Target Context # Activities
35981459 10.1016/j.ejmech.2022.114645 Human immunodeficiency virus 1 8
15115397 10.1021/jm030558s Human immunodeficiency virus 1 7
11527704 10.1016/s0960-894x(01)00411-5 Human immunodeficiency virus 1 5
11527705 10.1016/s0960-894x(01)00412-7 Human immunodeficiency virus 1 5
15771411 10.1021/jm040127p MT4 5
30223123 10.1016/j.ejmech.2018.09.013 Human immunodeficiency virus type 1 reverse transcriptase 5
15771441 10.1021/jm049439i ADMET 1
15771441 10.1021/jm049439i No relevant target 1

Data from ChEMBL 36 via Core Engine