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Assay Detail

CHEMBL5136571

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

Binding
Inhibition of human RIPK2 incubated for 120 mins in presence of [gamma33P]ATP by scintillation counting based radiometry assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Discovery of Potent and Selective Receptor-Interacting Serine/Threonine Protein Kinase 2 (RIPK2) Inhibitors for the Treatment of Inflammatory Bowel Diseases (IBDs).
Yuan X, Chen Y, Tang M, Wei Y, Shi M, Yang Y, Zhou Y, Yang T, Liu J, Liu K, Deng D, Zhang C, Chen L.
J Med Chem (2022) 65 : 9312 -9327
PubMed 35709396 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 8.17 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5187454 1 9.10
CHEMBL5195615 1 8.80
CHEMBL5171377 1 8.62
CHEMBL5197634 1 8.52
CHEMBL5205764 1 8.41
CHEMBL5205532 1 8.40
CHEMBL5174069 1 8.38
CHEMBL5171074 1 8.28
CHEMBL5169942 1 8.23
CHEMBL5187179 1 8.22
CHEMBL5184606 1 8.20
CHEMBL5180091 1 8.19
CHEMBL5175396 1 8.17
CHEMBL5191232 1 8.10
CHEMBL5207306 1 8.05
CHEMBL5174176 1 7.97
CHEMBL5191796 1 7.97
CHEMBL5189173 1 7.93
CHEMBL5172982 1 7.81
CHEMBL5204246 1 7.78
CHEMBL5170201 1 7.73
CHEMBL5185309 1 7.68
CHEMBL5206121 1 7.47
CHEMBL5169652 1 -
CHEMBL5184501 1 -
CHEMBL5195124 1 -
CHEMBL5206318 1 -
CHEMBL5201038 1 -
CHEMBL5181298 1 -
CHEMBL5202296 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5187454 IC50 = 0.8 nM 9.10
CHEMBL5195615 IC50 = 1.6 nM 8.80
CHEMBL5171377 IC50 = 2.4 nM 8.62
CHEMBL5197634 IC50 = 3.0 nM 8.52
CHEMBL5205764 IC50 = 3.9 nM 8.41
CHEMBL5205532 IC50 = 4.0 nM 8.40
CHEMBL5174069 IC50 = 4.2 nM 8.38
CHEMBL5171074 IC50 = 5.2 nM 8.28
CHEMBL5169942 IC50 = 5.9 nM 8.23
CHEMBL5187179 IC50 = 6.0 nM 8.22
CHEMBL5184606 IC50 = 6.3 nM 8.20
CHEMBL5180091 IC50 = 6.4 nM 8.19
CHEMBL5175396 IC50 = 6.7 nM 8.17
CHEMBL5191232 IC50 = 7.9 nM 8.10
CHEMBL5207306 IC50 = 9.0 nM 8.05
CHEMBL5174176 IC50 = 10.7 nM 7.97
CHEMBL5191796 IC50 = 10.8 nM 7.97
CHEMBL5189173 IC50 = 11.7 nM 7.93
CHEMBL5172982 IC50 = 15.6 nM 7.81
CHEMBL5204246 IC50 = 16.7 nM 7.78
CHEMBL5170201 IC50 = 18.5 nM 7.73
CHEMBL5185309 IC50 = 21.1 nM 7.68
CHEMBL5206121 IC50 = 33.8 nM 7.47
CHEMBL5169652 IC50 - -
CHEMBL5184501 IC50 - -
CHEMBL5195124 IC50 - -
CHEMBL5206318 IC50 - -
CHEMBL5201038 IC50 - -
CHEMBL5181298 IC50 - -
CHEMBL5202296 IC50 - -
CHEMBL5176553 IC50 - -
CHEMBL5191523 IC50 - -
CHEMBL5172451 IC50 - -
CHEMBL5174686 IC50 - -