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Assay Detail

CHEMBL4344882

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ADMET
Displacement of fluorescein labeled probe from full length human GST-tagged RIPK1 expressed in Sf9 cells incubated for 60 mins by HTRF assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Receptor-interacting serine/threonine-protein kinase 1 (CHEMBL5464)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage.
Hart AC, Abell L, Guo J, Mertzman ME, Padmanabha R, Macor JE, Chaudhry C, Lu H, O'Malley K, Shaw PJ, Weigelt C, Pokross M, Kish K, Kim KS, Cornelius L, Douglas AE, Calambur D, Zhang P, Carpenter B, Pitts WJ.
ACS Med Chem Lett (2020) 11 : 266 -271
PubMed 32184955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.64 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4470115 1 6.51
CHEMBL4434926 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4470115 IC50 = 310.0 nM 6.51
CHEMBL4434926 IC50 = 17000.0 nM 4.77