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Assay Detail

CHEMBL945966

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

Binding
Inhibition of HIV integrase strand transfer activity
8
Total Activities
8
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: potent and orally bioavailable C5-aza analogs.
Jin H, Wright M, Pastor R, Mish M, Metobo S, Jabri S, Lansdown R, Cai R, Pyun P, Tsiang M, Chen X, Kim CU.
Bioorg Med Chem Lett (2008) 18 : 1388 -1391
PubMed 18207398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.28 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254524 1 7.89
CHEMBL254316 RALTEGRAVIR 4.0 1 7.57
CHEMBL254318 1 7.55
CHEMBL209854 1 7.30
CHEMBL402290 1 7.21
CHEMBL254522 1 7.15
CHEMBL254317 1 7.00
CHEMBL254523 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL254524 IC50 = 13.0 nM 7.89
CHEMBL254316 RALTEGRAVIR IC50 = 27.0 nM 7.57
CHEMBL254318 IC50 = 28.0 nM 7.55
CHEMBL209854 IC50 = 50.0 nM 7.30
CHEMBL402290 IC50 = 62.0 nM 7.21
CHEMBL254522 IC50 = 71.0 nM 7.15
CHEMBL254317 IC50 = 100.0 nM 7.00
CHEMBL254523 IC50 = 265.0 nM 6.58