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Assay Detail

CHEMBL4135584

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

Binding
Inhibition of full length RIPK2 (unknown origin) pretreated for 30 mins followed by ATP addition measured after 2 hrs by ADP-d2 tracer based fluorescence assay
36
Total Activities
36
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

Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases.
He X, Da Ros S, Nelson J, Zhu X, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S, Jia Y, Bursulaya B, Kreusch A, Gao MY, Spraggon G, Baaten J, Clemmer L, Meeusen S, Huang D, Hill R, Nguyen-Tran V, Fathman J, Liu B, Tuntland T, Gordon P, Hollenbeck T, Ng K, Shi J, Bordone L, Liu H.
ACS Med Chem Lett (2017) 8 : 1048 -1053
PubMed 29057049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 7.49 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4176853 1 8.70
CHEMBL4161327 1 8.52
CHEMBL4171924 1 8.52
CHEMBL4173493 1 8.30
CHEMBL4161723 1 8.30
CHEMBL4160817 1 8.30
CHEMBL4166239 1 8.22
CHEMBL4159424 1 8.15
CHEMBL4170048 1 8.15
CHEMBL4162788 1 8.10
CHEMBL4164217 1 8.05
CHEMBL4168738 1 7.96
CHEMBL4163484 1 7.80
CHEMBL4167668 1 7.70
CHEMBL4171039 1 7.68
CHEMBL4162913 1 7.62
CHEMBL4173646 1 7.54
CHEMBL4174187 1 7.46
CHEMBL4170854 1 7.42
CHEMBL4160116 1 7.40
CHEMBL4172092 1 7.35
CHEMBL4169652 1 7.24
CHEMBL4165728 1 7.22
CHEMBL4165019 1 7.16
CHEMBL4166371 1 7.05
CHEMBL4160433 1 6.92
CHEMBL4167365 1 6.89
CHEMBL4166930 1 6.80
CHEMBL4175635 1 6.75
CHEMBL4175533 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4176853 IC50 = 2.0 nM 8.70
CHEMBL4161327 IC50 = 3.0 nM 8.52
CHEMBL4171924 IC50 = 3.0 nM 8.52
CHEMBL4173493 IC50 = 5.0 nM 8.30
CHEMBL4161723 IC50 = 5.0 nM 8.30
CHEMBL4160817 IC50 = 5.0 nM 8.30
CHEMBL4166239 IC50 = 6.0 nM 8.22
CHEMBL4159424 IC50 = 7.0 nM 8.15
CHEMBL4170048 IC50 = 7.0 nM 8.15
CHEMBL4162788 IC50 = 8.0 nM 8.10
CHEMBL4164217 IC50 = 9.0 nM 8.05
CHEMBL4168738 IC50 = 11.0 nM 7.96
CHEMBL4163484 IC50 = 16.0 nM 7.80
CHEMBL4167668 IC50 = 20.0 nM 7.70
CHEMBL4171039 IC50 = 21.0 nM 7.68
CHEMBL4162913 IC50 = 24.0 nM 7.62
CHEMBL4173646 IC50 = 29.0 nM 7.54
CHEMBL4174187 IC50 = 35.0 nM 7.46
CHEMBL4170854 IC50 = 38.0 nM 7.42
CHEMBL4160116 IC50 = 40.0 nM 7.40
CHEMBL4172092 IC50 = 45.0 nM 7.35
CHEMBL4169652 IC50 = 58.0 nM 7.24
CHEMBL4165728 IC50 = 60.0 nM 7.22
CHEMBL4165019 IC50 = 70.0 nM 7.16
CHEMBL4166371 IC50 = 90.0 nM 7.05
CHEMBL4160433 IC50 = 120.0 nM 6.92
CHEMBL4167365 IC50 = 130.0 nM 6.89
CHEMBL4166930 IC50 = 160.0 nM 6.80
CHEMBL4175635 IC50 = 180.0 nM 6.75
CHEMBL4175533 IC50 = 200.0 nM 6.70
CHEMBL4159032 IC50 = 430.0 nM 6.37
CHEMBL4170760 IC50 = 460.0 nM 6.34
CHEMBL4164029 IC50 = 520.0 nM 6.28
CHEMBL1078785 IC50 = 1500.0 nM 5.82
CHEMBL4174288 IC50 > 10000.0 nM -
CHEMBL4175235 IC50 > 10000.0 nM -