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Assay Detail

CHEMBL5576423

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

Binding
Inhibition of SARS-Cov-2 MPro assessed as inhibition constant by FRET assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Severe acute respiratory syndrome coronavirus 2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Replicase polyprotein 1ab (CHEMBL4523582)
Type SINGLE PROTEIN
Organism Severe acute respiratory syndrome coronavirus 2

Publication

A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19.
Allerton CMN, Arcari JT, Aschenbrenner LM, Avery M, Bechle BM, Behzadi MA, Boras B, Buzon LM, Cardin RD, Catlin NR, Carlo AA, Coffman KJ, Dantonio A, Di L, Eng H, Farley KA, Ferre RA, Gernhardt SS, Gibson SA, Greasley SE, Greenfield SR, Hurst BL, Kalgutkar AS, Kimoto E, Lanyon LF, Lovett GH, Lian Y, Liu W, Martínez Alsina LA, Noell S, Obach RS, Owen DR, Patel NC, Rai DK, Reese MR, Rothan HA, Sakata S, Sammons MF, Sathish JG, Sharma R, Steppan CM, Tuttle JB, Verhoest PR, Wei L, Yang Q, Yurgelonis I, Zhu Y.
J Med Chem (2024) 67 : 13550 -13571
PubMed 38687966 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.65 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5592467 1 9.77
CHEMBL5592186 1 9.20
CHEMBL5592632 1 9.15
CHEMBL5088846 1 8.95
CHEMBL5590130 1 8.95
CHEMBL5591580 IBUZATRELVIR 2.0 1 8.61
CHEMBL5595506 1 8.55
CHEMBL4802135 NIRMATRELVIR 4.0 1 8.51
CHEMBL5590851 1 8.41
CHEMBL5090635 1 8.35
CHEMBL5084811 1 8.26
CHEMBL5592077 1 7.89
CHEMBL5595086 1 7.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5592467 Ki = 0.17 nM 9.77
CHEMBL5592186 Ki = 0.63 nM 9.20
CHEMBL5592632 Ki = 0.71 nM 9.15
CHEMBL5088846 Ki = 1.12 nM 8.95
CHEMBL5590130 Ki = 1.13 nM 8.95
CHEMBL5591580 IBUZATRELVIR Ki = 2.48 nM 8.61
CHEMBL5595506 Ki = 2.83 nM 8.55
CHEMBL4802135 NIRMATRELVIR Ki = 3.11 nM 8.51
CHEMBL5590851 Ki = 3.88 nM 8.41
CHEMBL5090635 Ki = 4.46 nM 8.35
CHEMBL5084811 Ki = 5.49 nM 8.26
CHEMBL5592077 Ki = 13.0 nM 7.89
CHEMBL5595086 Ki = 13.27 nM 7.88