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Assay Detail

CHEMBL929986

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

Binding
Inhibition of HTLV1 protease L40I mutant expressed in Escherichia coli BL21(DE3)pLysS
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human T-cell leukemia virus type I
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Gag-Pro polyprotein (CHEMBL3346)
Type SINGLE PROTEIN
Organism Human T-cell leukemia virus 1 (strain Japan ATK-1 subtype A) (HTLV-1)

Publication

Truncation and non-natural amino acid substitution studies on HTLV-I protease hexapeptidic inhibitors.
Nguyen JT, Zhang M, Kumada HO, Itami A, Nishiyama K, Kimura T, Cheng M, Hayashi Y, Kiso Y.
Bioorg Med Chem Lett (2008) 18 : 366 -370
PubMed 18006315 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.82 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272710 1 7.08
CHEMBL271706 1 7.06
CHEMBL272280 1 7.02
CHEMBL271878 1 7.00
CHEMBL403182 1 6.99
CHEMBL404702 1 6.99
CHEMBL403240 1 6.97
CHEMBL256022 1 6.95
CHEMBL403770 1 6.91
CHEMBL256587 1 6.88
CHEMBL401718 1 6.85
CHEMBL271454 1 6.84
CHEMBL272920 1 6.84
CHEMBL404836 1 6.84
CHEMBL436816 1 6.82
CHEMBL257647 1 6.80
CHEMBL256385 1 6.80
CHEMBL233025 1 6.80
CHEMBL402525 1 6.75
CHEMBL401814 1 6.75
CHEMBL256588 1 6.71
CHEMBL256386 1 6.70
CHEMBL257649 1 6.60
CHEMBL272494 1 6.50
CHEMBL233649 1 6.45
CHEMBL258157 1 6.33
CHEMBL430094 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272710 IC50 = 84.0 nM 7.08
CHEMBL271706 IC50 = 88.0 nM 7.06
CHEMBL272280 IC50 = 95.0 nM 7.02
CHEMBL271878 IC50 = 101.0 nM 7.00
CHEMBL403182 IC50 = 102.0 nM 6.99
CHEMBL404702 IC50 = 103.0 nM 6.99
CHEMBL403240 IC50 = 107.0 nM 6.97
CHEMBL256022 IC50 = 113.0 nM 6.95
CHEMBL403770 IC50 = 123.0 nM 6.91
CHEMBL256587 IC50 = 131.0 nM 6.88
CHEMBL401718 IC50 = 140.0 nM 6.85
CHEMBL271454 IC50 = 146.0 nM 6.84
CHEMBL272920 IC50 = 145.0 nM 6.84
CHEMBL404836 IC50 = 144.0 nM 6.84
CHEMBL436816 IC50 = 152.0 nM 6.82
CHEMBL257647 IC50 = 160.0 nM 6.80
CHEMBL256385 IC50 = 159.0 nM 6.80
CHEMBL233025 IC50 = 159.0 nM 6.80
CHEMBL402525 IC50 = 180.0 nM 6.75
CHEMBL401814 IC50 = 180.0 nM 6.75
CHEMBL256588 IC50 = 193.0 nM 6.71
CHEMBL256386 IC50 = 201.0 nM 6.70
CHEMBL257649 IC50 = 249.0 nM 6.60
CHEMBL272494 IC50 = 320.0 nM 6.50
CHEMBL233649 IC50 = 353.0 nM 6.45
CHEMBL258157 IC50 = 473.0 nM 6.33
CHEMBL430094 IC50 > 1000.0 nM -