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Assay Detail

CHEMBL802762

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

Binding
In vitro inhibitory concentration against reverse transcriptase of HIV-1 (RT)
34
Total Activities
33
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 Expert

Target

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

Publication

Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
Livermore DG, Bethell RC, Cammack N, Hancock AP, Hann MM, Green DV, Lamont RB, Noble SA, Orr DC, Payne JJ.
J Med Chem (1993) 36 : 3784 -3794
PubMed 7504733 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.11 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL338099 1 9.22
CHEMBL341350 1 7.30
CHEMBL125446 1 7.10
CHEMBL1203237 1 7.10
CHEMBL434441 1 7.00
CHEMBL125532 1 7.00
CHEMBL121820 1 6.64
CHEMBL341512 1 6.57
CHEMBL125205 1 6.47
CHEMBL125084 1 6.42
CHEMBL127427 1 6.26
CHEMBL340248 1 6.25
CHEMBL435017 1 6.19
CHEMBL1203236 1 6.19
CHEMBL124248 1 6.08
CHEMBL338415 1 5.89
CHEMBL338339 2 5.89
CHEMBL123514 1 5.70
CHEMBL435216 1 5.64
CHEMBL123202 1 5.60
CHEMBL126216 1 5.58
CHEMBL126811 1 5.52
CHEMBL338823 1 5.52
CHEMBL124271 1 5.47
CHEMBL338302 1 5.47
CHEMBL332351 1 5.41
CHEMBL124246 1 5.32
CHEMBL262415 1 5.17
CHEMBL341238 1 4.85
CHEMBL123839 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL338099 IC50 = 0.6 nM 9.22
CHEMBL341350 IC50 = 50.0 nM 7.30
CHEMBL125446 IC50 = 80.0 nM 7.10
CHEMBL1203237 IC50 = 80.0 nM 7.10
CHEMBL434441 IC50 = 100.0 nM 7.00
CHEMBL125532 IC50 = 100.0 nM 7.00
CHEMBL121820 IC50 = 230.0 nM 6.64
CHEMBL341512 IC50 = 270.0 nM 6.57
CHEMBL125205 IC50 = 340.0 nM 6.47
CHEMBL125084 IC50 = 380.0 nM 6.42
CHEMBL127427 IC50 = 550.0 nM 6.26
CHEMBL340248 IC50 = 560.0 nM 6.25
CHEMBL435017 IC50 = 640.0 nM 6.19
CHEMBL1203236 IC50 = 640.0 nM 6.19
CHEMBL124248 IC50 = 840.0 nM 6.08
CHEMBL338415 IC50 = 1300.0 nM 5.89
CHEMBL338339 IC50 = 1300.0 nM 5.89
CHEMBL338339 IC50 = 1340.0 nM 5.87
CHEMBL123514 IC50 = 2000.0 nM 5.70
CHEMBL435216 IC50 = 2300.0 nM 5.64
CHEMBL123202 IC50 = 2500.0 nM 5.60
CHEMBL126216 IC50 = 2600.0 nM 5.58
CHEMBL126811 IC50 = 3000.0 nM 5.52
CHEMBL338823 IC50 = 3000.0 nM 5.52
CHEMBL124271 IC50 = 3400.0 nM 5.47
CHEMBL338302 IC50 = 3400.0 nM 5.47
CHEMBL332351 IC50 = 3900.0 nM 5.41
CHEMBL124246 IC50 = 4800.0 nM 5.32
CHEMBL262415 IC50 = 6700.0 nM 5.17
CHEMBL341238 IC50 = 14000.0 nM 4.85
CHEMBL123839 IC50 = 22000.0 nM 4.66
CHEMBL434047 IC50 = 110000.0 nM -
CHEMBL125806 IC50 = 110000.0 nM -
CHEMBL333863 IC50 > 100000.0 nM -