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Assay Detail

CHEMBL2345503

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

Binding
Inhibition of HIV1 reverse transcriptase after 1 hr by colorimetric assay
26
Total Activities
26
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 pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors (NNRTIs) with high potency against NNRTI-resistant HIV-1 strains.
Li A, Ouyang Y, Wang Z, Cao Y, Liu X, Ran L, Li C, Li L, Zhang L, Qiao K, Xu W, Huang Y, Zhang Z, Tian C, Liu Z, Jiang S, Shao Y, Du Y, Ma L, Wang X, Liu J.
J Med Chem (2013) 56 : 3593 -3608
PubMed 23540737 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.00 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2337416 1 8.52
CHEMBL2337437 1 8.00
CHEMBL2337432 1 7.48
CHEMBL2337433 1 7.23
CHEMBL436546 1 7.06
CHEMBL2337430 1 6.89
CHEMBL2337436 1 6.82
CHEMBL2337431 1 6.80
CHEMBL2337429 1 6.39
CHEMBL2337428 1 6.23
CHEMBL2337435 1 6.19
CHEMBL2337427 1 5.92
CHEMBL2337438 1 5.88
CHEMBL57 NEVIRAPINE 4.0 1 5.35
CHEMBL2331616 1 5.28
CHEMBL2337421 1 4.70
CHEMBL2337422 1 4.48
CHEMBL2337423 1 4.43
CHEMBL2337426 1 4.23
CHEMBL2337424 1 4.13
CHEMBL2337418 1 4.09
CHEMBL2337425 1 -
CHEMBL2337434 1 -
CHEMBL2337420 1 -
CHEMBL2337419 1 -
CHEMBL2337417 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2337416 IC50 = 3.0 nM 8.52
CHEMBL2337437 IC50 = 10.0 nM 8.00
CHEMBL2337432 IC50 = 33.0 nM 7.48
CHEMBL2337433 IC50 = 59.0 nM 7.23
CHEMBL436546 IC50 = 88.0 nM 7.06
CHEMBL2337430 IC50 = 130.0 nM 6.89
CHEMBL2337436 IC50 = 150.0 nM 6.82
CHEMBL2337431 IC50 = 160.0 nM 6.80
CHEMBL2337429 IC50 = 410.0 nM 6.39
CHEMBL2337428 IC50 = 590.0 nM 6.23
CHEMBL2337435 IC50 = 650.0 nM 6.19
CHEMBL2337427 IC50 = 1210.0 nM 5.92
CHEMBL2337438 IC50 = 1310.0 nM 5.88
CHEMBL57 NEVIRAPINE IC50 = 4450.0 nM 5.35
CHEMBL2331616 IC50 = 5290.0 nM 5.28
CHEMBL2337421 IC50 = 19810.0 nM 4.70
CHEMBL2337422 IC50 = 32880.0 nM 4.48
CHEMBL2337423 IC50 = 37070.0 nM 4.43
CHEMBL2337426 IC50 = 59300.0 nM 4.23
CHEMBL2337424 IC50 = 73540.0 nM 4.13
CHEMBL2337418 IC50 = 80990.0 nM 4.09
CHEMBL2337425 IC50 > 100000.0 nM -
CHEMBL2337434 IC50 > 100000.0 nM -
CHEMBL2337420 IC50 > 100000.0 nM -
CHEMBL2337419 IC50 > 100000.0 nM -
CHEMBL2337417 IC50 > 100000.0 nM -