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Assay Detail

CHEMBL2318921

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

Binding
Inhibition of SARS coronavirus 3C-like protease R188I mutant using Dabcyl- KTSAVLQSGFRKME-Edans as substrate by fluorescence spectrophotometry
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Severe acute respiratory syndrome-related coronavirus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Design and synthesis of new tripeptide-type SARS-CoV 3CL protease inhibitors containing an electrophilic arylketone moiety.
Konno S, Thanigaimalai P, Yamamoto T, Nakada K, Kakiuchi R, Takayama K, Yamazaki Y, Yakushiji F, Akaji K, Kiso Y, Kawasaki Y, Chen SE, Freire E, Hayashi Y.
Bioorg Med Chem (2013) 21 : 412 -424
PubMed 23245752 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 6.67 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2316753 1 8.52
CHEMBL2316746 1 8.39
CHEMBL2316751 1 7.96
CHEMBL2316748 1 7.85
CHEMBL2316747 1 7.66
CHEMBL2316450 1 7.22
CHEMBL2316457 1 6.77
CHEMBL2316460 1 6.66
CHEMBL2316459 1 6.66
CHEMBL2316451 1 6.57
CHEMBL2316458 1 6.48
CHEMBL2316456 1 6.33
CHEMBL2316454 1 5.89
CHEMBL2316452 1 5.84
CHEMBL539209 1 5.66
CHEMBL2316455 1 4.66
CHEMBL2316453 1 4.25
CHEMBL2316741 1 -
CHEMBL2316742 1 -
CHEMBL2316743 1 -
CHEMBL2316756 1 -
CHEMBL2316465 1 -
CHEMBL2316464 1 -
CHEMBL2316744 1 -
CHEMBL2316745 1 -
CHEMBL2316749 1 -
CHEMBL2316750 1 -
CHEMBL2316752 1 -
CHEMBL2316754 1 -
CHEMBL2316755 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2316753 Ki = 3.0 nM 8.52
CHEMBL2316746 Ki = 4.1 nM 8.39
CHEMBL2316751 Ki = 11.0 nM 7.96
CHEMBL2316748 Ki = 14.0 nM 7.85
CHEMBL2316747 Ki = 22.0 nM 7.66
CHEMBL2316450 Ki = 60.0 nM 7.22
CHEMBL2316457 Ki = 170.0 nM 6.77
CHEMBL2316460 Ki = 220.0 nM 6.66
CHEMBL2316459 Ki = 220.0 nM 6.66
CHEMBL2316451 Ki = 270.0 nM 6.57
CHEMBL2316458 Ki = 330.0 nM 6.48
CHEMBL2316456 Ki = 470.0 nM 6.33
CHEMBL2316454 Ki = 1300.0 nM 5.89
CHEMBL2316452 Ki = 1460.0 nM 5.84
CHEMBL539209 Ki = 2200.0 nM 5.66
CHEMBL2316455 Ki = 22000.0 nM 4.66
CHEMBL2316453 Ki = 56000.0 nM 4.25
CHEMBL2316741 Ki - -
CHEMBL2316742 Ki - -
CHEMBL2316743 Ki - -
CHEMBL2316756 Ki - -
CHEMBL2316465 Ki - -
CHEMBL2316464 Ki - -
CHEMBL2316744 Ki - -
CHEMBL2316745 Ki - -
CHEMBL2316749 Ki - -
CHEMBL2316750 Ki - -
CHEMBL2316752 Ki - -
CHEMBL2316754 Ki - -
CHEMBL2316755 Ki - -
CHEMBL2316461 Ki - -