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Assay Detail

CHEMBL804266

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

Binding
Inhibition of reverse transcriptase of HIV-1 (strain RF)-infected MT-4 cells in RPMI 1640 growth medium in MTM assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Cell Type MT4
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
EC50 30 6.37 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 8.52
CHEMBL268871 L-697661 1 8.15
CHEMBL434441 1 8.00
CHEMBL338099 1 8.00
CHEMBL125446 1 7.70
CHEMBL127427 1 6.40
CHEMBL125532 1 6.36
CHEMBL340248 1 6.23
CHEMBL1203237 1 6.20
CHEMBL123202 1 6.16
CHEMBL435017 1 6.14
CHEMBL338339 1 6.11
CHEMBL125084 1 6.07
CHEMBL338823 1 6.05
CHEMBL125205 1 6.00
CHEMBL126216 1 5.96
CHEMBL435216 1 5.89
CHEMBL341512 1 5.75
CHEMBL1203236 1 5.03
CHEMBL126811 1 4.60
CHEMBL332351 1 4.55
CHEMBL338302 1 -
CHEMBL338415 1 -
CHEMBL124271 1 -
CHEMBL341238 1 -
CHEMBL123514 1 -
CHEMBL121820 1 -
CHEMBL124246 1 -
CHEMBL124248 1 -
CHEMBL123839 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 3.0 nM 8.52
CHEMBL268871 L-697661 EC50 = 7.0 nM 8.15
CHEMBL434441 EC50 = 10.0 nM 8.00
CHEMBL338099 EC50 = 10.0 nM 8.00
CHEMBL125446 EC50 = 20.0 nM 7.70
CHEMBL127427 EC50 = 400.0 nM 6.40
CHEMBL125532 EC50 = 440.0 nM 6.36
CHEMBL340248 EC50 = 590.0 nM 6.23
CHEMBL1203237 EC50 = 630.0 nM 6.20
CHEMBL123202 EC50 = 700.0 nM 6.16
CHEMBL435017 EC50 = 720.0 nM 6.14
CHEMBL338339 EC50 = 780.0 nM 6.11
CHEMBL125084 EC50 = 860.0 nM 6.07
CHEMBL338823 EC50 = 890.0 nM 6.05
CHEMBL125205 EC50 = 1000.0 nM 6.00
CHEMBL126216 EC50 = 1100.0 nM 5.96
CHEMBL435216 EC50 = 1300.0 nM 5.89
CHEMBL341512 EC50 = 1800.0 nM 5.75
CHEMBL1203236 EC50 = 9300.0 nM 5.03
CHEMBL126811 EC50 = 25000.0 nM 4.60
CHEMBL332351 EC50 = 28000.0 nM 4.55
CHEMBL338302 EC50 > 25000.0 nM -
CHEMBL338415 EC50 > 260000.0 nM -
CHEMBL124271 EC50 > 25000.0 nM -
CHEMBL341238 EC50 > 250000.0 nM -
CHEMBL123514 EC50 > 25000.0 nM -
CHEMBL121820 EC50 < 30.0 nM -
CHEMBL124246 EC50 > 250000.0 nM -
CHEMBL124248 EC50 < 30.0 nM -
CHEMBL123839 EC50 > 250000.0 nM -