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Assay Detail

CHEMBL5583145

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

Binding
Binding affinity to 6his-tagged CHIKV nsP2 (1009 to 1329 residues) extracted from Escherichia coli Rosetta2 (DE3) cells assessed as inhibition constant measured over 45 mins
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Chikungunya virus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Polyprotein P1234 (CHEMBL4295622)
Type SINGLE PROTEIN
Organism Chikungunya virus (strain S27-African prototype) (CHIKV)

Publication

Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors of <i>Chikungunya</i> nsP2 Cysteine Protease with Antialphavirus Activity.
Ghoshal A, Asressu KH, Hossain MA, Brown PJ, Nandakumar M, Vala A, Merten EM, Sears JD, Law I, Burdick JE, Morales NL, Perveen S, Pearce KH, Popov KI, Moorman NJ, Heise MT, Willson TM.
J Med Chem (2024) 67 : 16505 -16532
PubMed 39235978 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.36 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5593311 1 7.40
CHEMBL5592235 1 7.20
CHEMBL5591218 1 7.20
CHEMBL5594820 1 7.00
CHEMBL5594389 1 6.70
CHEMBL5594644 1 6.60
CHEMBL5592413 1 6.50
CHEMBL5590710 1 6.50
CHEMBL5593604 1 6.50
CHEMBL5593893 1 6.30
CHEMBL5592232 1 6.20
CHEMBL5595846 1 6.10
CHEMBL5595202 1 6.10
CHEMBL5592794 1 6.10
CHEMBL5583848 1 5.80
CHEMBL5583713 1 5.80
CHEMBL5595857 1 5.70
CHEMBL5594235 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5593311 Ki = 39.81 nM 7.40
CHEMBL5592235 Ki = 63.1 nM 7.20
CHEMBL5591218 Ki = 63.1 nM 7.20
CHEMBL5594820 Ki = 100.0 nM 7.00
CHEMBL5594389 Ki = 199.53 nM 6.70
CHEMBL5594644 Ki = 251.19 nM 6.60
CHEMBL5592413 Ki = 316.23 nM 6.50
CHEMBL5590710 Ki = 316.23 nM 6.50
CHEMBL5593604 Ki = 316.23 nM 6.50
CHEMBL5593893 Ki = 501.19 nM 6.30
CHEMBL5592232 Ki = 630.96 nM 6.20
CHEMBL5595846 Ki = 794.33 nM 6.10
CHEMBL5595202 Ki = 794.33 nM 6.10
CHEMBL5592794 Ki = 794.33 nM 6.10
CHEMBL5583848 Ki = 1584.89 nM 5.80
CHEMBL5583713 Ki = 1584.89 nM 5.80
CHEMBL5595857 Ki = 1995.26 nM 5.70
CHEMBL5594235 Ki = 15848.93 nM 4.80