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Assay Detail

CHEMBL4195748

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

Binding
Inhibition of NIK (unknown origin) expressed in baculovirus infected insect cells assessed as reduction in hydrolysis of ATP to ADP after 1 to 2 hrs by ADP-MR121 633 tracer based fluorescence polarization assay
23
Total Activities
23
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

Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase.
Blaquiere N, Castanedo GM, Burch JD, Berezhkovskiy LM, Brightbill H, Brown S, Chan C, Chiang PC, Crawford JJ, Dong T, Fan P, Feng J, Ghilardi N, Godemann R, Gogol E, Grabbe A, Hole AJ, Hu B, Hymowitz SG, Alaoui Ismaili MH, Le H, Lee P, Lee W, Lin X, Liu N, McEwan PA, McKenzie B, Silvestre HL, Suto E, Sujatha-Bhaskar S, Wu G, Wu LC, Zhang Y, Zhong Z, Staben ST.
J Med Chem (2018) 61 : 6801 -6813
PubMed 29940120 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 9.02 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205698 1 10.30
CHEMBL4216289 1 10.15
CHEMBL4215425 1 10.15
CHEMBL4211046 1 10.10
CHEMBL4204233 1 9.89
CHEMBL4211551 1 9.77
CHEMBL4217407 1 9.74
CHEMBL4209095 1 9.64
CHEMBL4212052 1 9.64
CHEMBL4211840 1 9.64
CHEMBL4208337 1 9.57
CHEMBL4211560 1 9.38
CHEMBL4214032 1 9.23
CHEMBL4216004 1 9.07
CHEMBL4217923 1 8.89
CHEMBL4210461 1 8.70
CHEMBL4205172 1 8.33
CHEMBL4210066 1 8.23
CHEMBL4203779 1 8.03
CHEMBL4215454 1 7.80
CHEMBL4203279 1 7.55
CHEMBL4212983 1 7.17
CHEMBL4206671 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205698 Ki = 0.05 nM 10.30
CHEMBL4216289 Ki = 0.07 nM 10.15
CHEMBL4215425 Ki = 0.07 nM 10.15
CHEMBL4211046 Ki = 0.08 nM 10.10
CHEMBL4204233 Ki = 0.13 nM 9.89
CHEMBL4211551 Ki = 0.17 nM 9.77
CHEMBL4217407 Ki = 0.18 nM 9.74
CHEMBL4209095 Ki = 0.23 nM 9.64
CHEMBL4212052 Ki = 0.23 nM 9.64
CHEMBL4211840 Ki = 0.23 nM 9.64
CHEMBL4208337 Ki = 0.27 nM 9.57
CHEMBL4211560 Ki = 0.42 nM 9.38
CHEMBL4214032 Ki = 0.59 nM 9.23
CHEMBL4216004 Ki = 0.86 nM 9.07
CHEMBL4217923 Ki = 1.3 nM 8.89
CHEMBL4210461 Ki = 2.0 nM 8.70
CHEMBL4205172 Ki = 4.7 nM 8.33
CHEMBL4210066 Ki = 5.9 nM 8.23
CHEMBL4203779 Ki = 9.4 nM 8.03
CHEMBL4215454 Ki = 16.0 nM 7.80
CHEMBL4203279 Ki = 28.0 nM 7.55
CHEMBL4212983 Ki = 68.0 nM 7.17
CHEMBL4206671 Ki = 350.0 nM 6.46