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Assay Detail

CHEMBL994471

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

Binding
Inhibition of HIV1 reverse transcriptase RNA-dependent DNA polymerase activity assessed as incorporation of radioactive dTTP into poly(rA)/oligo(DT)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
Monforte AM, Rao A, Logoteta P, Ferro S, De Luca L, Barreca ML, Iraci N, Maga G, De Clercq E, Pannecouque C, Chimirri A.
Bioorg Med Chem (2008) 16 : 7429 -7435
PubMed 18585918 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.69 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477192 1 8.52
CHEMBL223228 EFAVIRENZ 4.0 1 8.40
CHEMBL234401 1 8.30
CHEMBL450764 1 7.77
CHEMBL506852 1 7.34
CHEMBL443883 1 7.00
CHEMBL479069 1 7.00
CHEMBL518737 1 7.00
CHEMBL515189 1 6.85
CHEMBL234400 1 6.82
CHEMBL514396 1 6.80
CHEMBL444417 1 6.80
CHEMBL57 NEVIRAPINE 4.0 1 6.75
CHEMBL478236 1 6.70
CHEMBL443879 1 6.55
CHEMBL393003 1 6.16
CHEMBL447646 1 5.89
CHEMBL507975 1 4.52
CHEMBL477602 1 4.42
CHEMBL477603 1 4.11
CHEMBL518738 1 -
CHEMBL479068 1 -
CHEMBL478235 1 -
CHEMBL516423 1 -
CHEMBL514527 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477192 IC50 = 3.0 nM 8.52
CHEMBL223228 EFAVIRENZ IC50 = 4.0 nM 8.40
CHEMBL234401 IC50 = 5.0 nM 8.30
CHEMBL450764 IC50 = 17.0 nM 7.77
CHEMBL506852 IC50 = 46.0 nM 7.34
CHEMBL443883 IC50 = 100.0 nM 7.00
CHEMBL479069 IC50 = 100.0 nM 7.00
CHEMBL518737 IC50 = 100.0 nM 7.00
CHEMBL515189 IC50 = 140.0 nM 6.85
CHEMBL234400 IC50 = 150.0 nM 6.82
CHEMBL514396 IC50 = 158.0 nM 6.80
CHEMBL444417 IC50 = 160.0 nM 6.80
CHEMBL57 NEVIRAPINE IC50 = 180.0 nM 6.75
CHEMBL478236 IC50 = 200.0 nM 6.70
CHEMBL443879 IC50 = 280.0 nM 6.55
CHEMBL393003 IC50 = 700.0 nM 6.16
CHEMBL447646 IC50 = 1300.0 nM 5.89
CHEMBL507975 IC50 = 30000.0 nM 4.52
CHEMBL477602 IC50 = 38500.0 nM 4.42
CHEMBL477603 IC50 = 76920.0 nM 4.11
CHEMBL518738 IC50 > 100000.0 nM -
CHEMBL479068 IC50 > 100000.0 nM -
CHEMBL478235 IC50 > 400000.0 nM -
CHEMBL516423 IC50 > 100000.0 nM -
CHEMBL514527 IC50 > 100000.0 nM -