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Assay Detail

CHEMBL802760

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro inhibitory activity against HIV-1 RT in CEM4 cell line
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Cell Type CEM4
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Synthesis of non-immunosuppressive cyclophilin-Binding cyclosporin A derivatives as potential anti-HIV-1 drugs.
Evers M, Barrière JC, Bashiardes G, Bousseau A, Carry JC, Dereu N, Filoche B, Henin Y, Sablé S, Vuilhorgne M, Mignani S.
Bioorg Med Chem Lett (2003) 13 : 4415 -4419
PubMed 14643337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.24 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2407581 1 8.60
CHEMBL3038082 1 7.71
CHEMBL3038084 1 7.71
CHEMBL3038085 1 7.62
CHEMBL3038081 1 7.46
CHEMBL3038083 1 7.37
CHEMBL1269597 SCY 635 2.0 1 7.35
CHEMBL3038090 1 7.33
CHEMBL3038087 1 7.18
CHEMBL3038089 1 7.16
CHEMBL3038088 1 7.14
CHEMBL3038086 1 7.10
CHEMBL3038092 1 7.09
CHEMBL2407585 1 7.08
CHEMBL405301 1 7.02
CHEMBL3038093 1 7.00
CHEMBL442519 1 6.86
CHEMBL3038091 1 6.53
CHEMBL160 CYCLOSPORINE 4.0 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2407581 IC50 = 2.5 nM 8.60
CHEMBL3038082 IC50 = 19.5 nM 7.71
CHEMBL3038084 IC50 = 19.5 nM 7.71
CHEMBL3038085 IC50 = 24.0 nM 7.62
CHEMBL3038081 IC50 = 35.0 nM 7.46
CHEMBL3038083 IC50 = 43.0 nM 7.37
CHEMBL1269597 SCY 635 IC50 = 45.0 nM 7.35
CHEMBL3038090 IC50 = 47.0 nM 7.33
CHEMBL3038087 IC50 = 65.5 nM 7.18
CHEMBL3038089 IC50 = 70.0 nM 7.16
CHEMBL3038088 IC50 = 72.0 nM 7.14
CHEMBL3038086 IC50 = 80.0 nM 7.10
CHEMBL3038092 IC50 = 80.5 nM 7.09
CHEMBL2407585 IC50 = 84.0 nM 7.08
CHEMBL405301 IC50 = 95.0 nM 7.02
CHEMBL3038093 IC50 = 101.0 nM 7.00
CHEMBL442519 IC50 = 137.5 nM 6.86
CHEMBL3038091 IC50 = 293.0 nM 6.53
CHEMBL160 CYCLOSPORINE IC50 = 455.0 nM 6.34