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Assay Detail

CHEMBL956746

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Binding
Inhibition of HIV integrase strand transfer activity
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Tricyclic HIV integrase inhibitors V. SAR studies on the benzyl moiety.
Jin H, Metobo S, Jabri S, Mish M, Lansdown R, Chen X, Tsiang M, Wright M, Kim CU.
Bioorg Med Chem Lett (2009) 19 : 2263 -2265
PubMed 19285389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.34 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL470418 1 8.30
CHEMBL513189 1 7.55
CHEMBL469365 1 7.41
CHEMBL254316 RALTEGRAVIR 4.0 1 7.40
CHEMBL513363 1 7.28
CHEMBL451850 1 7.21
CHEMBL470417 1 7.13
CHEMBL469356 1 6.92
CHEMBL512324 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL470418 IC50 = 5.0 nM 8.30
CHEMBL513189 IC50 = 28.0 nM 7.55
CHEMBL469365 IC50 = 39.0 nM 7.41
CHEMBL254316 RALTEGRAVIR IC50 = 40.0 nM 7.40
CHEMBL513363 IC50 = 52.0 nM 7.28
CHEMBL451850 IC50 = 61.0 nM 7.21
CHEMBL470417 IC50 = 74.0 nM 7.13
CHEMBL469356 IC50 = 120.0 nM 6.92
CHEMBL512324 IC50 = 135.0 nM 6.87