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Assay Detail

CHEMBL4344884

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

ADMET
Displacement of fluorescein labeled ATP probe from His/GST-tagged RIPK2 (unknown origin) incubated for 60 mins by HTRF assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Receptor-interacting serine/threonine-protein kinase 2 (CHEMBL5014)
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 11 5.57 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4476485 1 6.17
CHEMBL4455682 1 5.75
CHEMBL4552106 1 5.52
CHEMBL4476076 1 5.51
CHEMBL4542026 1 4.89
CHEMBL509101 1 -
CHEMBL4572309 1 -
CHEMBL4468222 1 -
CHEMBL4434881 1 -
CHEMBL4438939 1 -
CHEMBL4551490 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4476485 IC50 = 680.0 nM 6.17
CHEMBL4455682 IC50 = 1800.0 nM 5.75
CHEMBL4552106 IC50 = 3000.0 nM 5.52
CHEMBL4476076 IC50 = 3100.0 nM 5.51
CHEMBL4542026 IC50 = 13000.0 nM 4.89
CHEMBL509101 IC50 > 15000.0 nM -
CHEMBL4572309 IC50 > 15000.0 nM -
CHEMBL4468222 IC50 > 15000.0 nM -
CHEMBL4434881 IC50 > 15000.0 nM -
CHEMBL4438939 IC50 > 15000.0 nM -
CHEMBL4551490 IC50 > 10000.0 nM -