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Assay Detail

CHEMBL4825906

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

Binding
Inhibition of Respiratory syncytial virus A2 fusion protein expressed in HEK293T cells harboring GAL4-NF-kappaB assessed as reduction in cell-cell fusion by luciferase assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human respiratory syncytial virus A2
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Fusion glycoprotein F0 (CHEMBL3856166)
Type SINGLE PROTEIN
Organism Human respiratory syncytial virus A (strain A2)

Publication

Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion.
Cockerill GS, Angell RM, Bedernjak A, Chuckowree I, Fraser I, Gascon-Simorte J, Gilman MSA, Good JAD, Harland R, Johnson SM, Ludes-Meyers JH, Littler E, Lumley J, Lunn G, Mathews N, McLellan JS, Paradowski M, Peeples ME, Scott C, Tait D, Taylor G, Thom M, Thomas E, Villalonga Barber C, Ward SE, Watterson D, Williams G, Young P, Powell K.
J Med Chem (2021) 64 : 3658 -3676
PubMed 33729773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.13 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4469438 1 9.40
CHEMBL4878302 1 9.30
CHEMBL4872095 1 9.15
CHEMBL4297497 SISUNATOVIR 2.0 1 9.05
CHEMBL4867108 1 9.00
CHEMBL4865906 1 8.92
CHEMBL4874709 1 8.92
CHEMBL4860271 1 8.89
CHEMBL4853602 1 8.82
CHEMBL4863172 1 8.59
CHEMBL4873528 1 8.59
CHEMBL4855358 1 8.52
CHEMBL4872263 1 8.35
CHEMBL4876843 1 8.21
CHEMBL4862291 1 7.96
CHEMBL4859694 1 7.43
CHEMBL4878086 1 7.33
CHEMBL4847062 1 7.15
CHEMBL4866951 1 6.74
CHEMBL4871056 1 6.44
CHEMBL4869353 1 6.19
CHEMBL4873987 1 5.97
CHEMBL4850153 1 -
CHEMBL4878851 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4469438 IC50 = 0.4 nM 9.40
CHEMBL4878302 IC50 = 0.5 nM 9.30
CHEMBL4872095 IC50 = 0.7 nM 9.15
CHEMBL4297497 SISUNATOVIR IC50 = 0.9 nM 9.05
CHEMBL4867108 IC50 = 1.0 nM 9.00
CHEMBL4865906 IC50 = 1.2 nM 8.92
CHEMBL4874709 IC50 = 1.2 nM 8.92
CHEMBL4860271 IC50 = 1.3 nM 8.89
CHEMBL4853602 IC50 = 1.5 nM 8.82
CHEMBL4863172 IC50 = 2.6 nM 8.59
CHEMBL4873528 IC50 = 2.6 nM 8.59
CHEMBL4855358 IC50 = 3.0 nM 8.52
CHEMBL4872263 IC50 = 4.5 nM 8.35
CHEMBL4876843 IC50 = 6.2 nM 8.21
CHEMBL4862291 IC50 = 11.1 nM 7.96
CHEMBL4859694 IC50 = 37.2 nM 7.43
CHEMBL4878086 IC50 = 46.7 nM 7.33
CHEMBL4847062 IC50 = 71.0 nM 7.15
CHEMBL4866951 IC50 = 183.0 nM 6.74
CHEMBL4871056 IC50 = 364.5 nM 6.44
CHEMBL4869353 IC50 = 640.5 nM 6.19
CHEMBL4873987 IC50 = 1069.5 nM 5.97
CHEMBL4850153 IC50 - -
CHEMBL4878851 IC50 > 25000.0 nM -