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Assay Detail

CHEMBL4618345

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

Binding
Inhibition of recombinant N-terminal GST-fused human NIK (319 to 947 residues) expressed in baculovirus expression system incubated for 120 mins in presence of ATP by ADP-glo based luminescence 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

Mitogen-activated protein kinase kinase kinase 14 (CHEMBL5888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of N-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine Derivatives as Novel, Potent, and Selective NF-κB Inducing Kinase (NIK) Inhibitors for the Treatment of Psoriasis.
Zhu Y, Ma Y, Zu W, Song J, Wang H, Zhong Y, Li H, Zhang Y, Gao Q, Kong B, Xu J, Jiang F, Wang X, Li S, Liu C, Liu H, Lu T, Chen Y.
J Med Chem (2020) 63 : 6748 -6773
PubMed 32479083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 7.04 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3187788 1 8.33
CHEMBL4648033 1 8.18
CHEMBL4644825 1 8.09
CHEMBL4642561 1 8.06
CHEMBL4645565 1 8.01
CHEMBL4643621 1 7.94
CHEMBL4636517 1 7.92
CHEMBL4639487 1 7.82
CHEMBL4634128 1 7.79
CHEMBL4640754 1 7.75
CHEMBL4636885 1 7.65
CHEMBL4635451 1 7.46
CHEMBL4636048 1 7.32
CHEMBL4642847 1 7.30
CHEMBL4643185 1 7.22
CHEMBL4647027 1 7.16
CHEMBL4639818 1 7.14
CHEMBL4645354 1 7.11
CHEMBL4642207 1 6.97
CHEMBL4643436 1 6.95
CHEMBL4642063 1 6.87
CHEMBL4644359 1 6.75
CHEMBL4635397 1 6.70
CHEMBL4638853 1 6.68
CHEMBL4648928 1 6.32
CHEMBL4640652 1 6.19
CHEMBL4648213 1 6.15
CHEMBL4635659 1 5.90
CHEMBL4640245 1 5.86
CHEMBL4645612 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3187788 IC50 = 4.7 nM 8.33
CHEMBL4648033 IC50 = 6.59 nM 8.18
CHEMBL4644825 IC50 = 8.22 nM 8.09
CHEMBL4642561 IC50 = 8.63 nM 8.06
CHEMBL4645565 IC50 = 9.87 nM 8.01
CHEMBL4643621 IC50 = 11.4 nM 7.94
CHEMBL4636517 IC50 = 11.98 nM 7.92
CHEMBL4639487 IC50 = 15.3 nM 7.82
CHEMBL4634128 IC50 = 16.2 nM 7.79
CHEMBL4640754 IC50 = 17.8 nM 7.75
CHEMBL4636885 IC50 = 22.5 nM 7.65
CHEMBL4635451 IC50 = 34.5 nM 7.46
CHEMBL4636048 IC50 = 47.9 nM 7.32
CHEMBL4642847 IC50 = 50.4 nM 7.30
CHEMBL4643185 IC50 = 60.1 nM 7.22
CHEMBL4647027 IC50 = 69.16 nM 7.16
CHEMBL4639818 IC50 = 72.4 nM 7.14
CHEMBL4645354 IC50 = 78.3 nM 7.11
CHEMBL4642207 IC50 = 106.7 nM 6.97
CHEMBL4643436 IC50 = 112.0 nM 6.95
CHEMBL4642063 IC50 = 135.7 nM 6.87
CHEMBL4644359 IC50 = 179.0 nM 6.75
CHEMBL4635397 IC50 = 199.9 nM 6.70
CHEMBL4638853 IC50 = 209.5 nM 6.68
CHEMBL4648928 IC50 = 484.0 nM 6.32
CHEMBL4640652 IC50 = 645.0 nM 6.19
CHEMBL4648213 IC50 = 705.0 nM 6.15
CHEMBL4635659 IC50 = 1270.0 nM 5.90
CHEMBL4640245 IC50 = 1378.0 nM 5.86
CHEMBL4645612 IC50 = 1404.0 nM 5.85
CHEMBL4643512 IC50 = 1639.0 nM 5.79
CHEMBL4645639 IC50 = 2240.0 nM 5.65
CHEMBL4641000 IC50 = 2714.0 nM 5.57
CHEMBL4642638 IC50 > 10000.0 nM -
CHEMBL4632558 IC50 - -
CHEMBL4640623 IC50 - -