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Assay Detail

CHEMBL2346384

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

Binding
Inhibition of NIK (unknown origin) autophosphorylation after 1 hr by chemiluminescent assay
31
Total Activities
31
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

Inhibiting NF-κB-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures.
Li K, McGee LR, Fisher B, Sudom A, Liu J, Rubenstein SM, Anwer MK, Cushing TD, Shin Y, Ayres M, Lee F, Eksterowicz J, Faulder P, Waszkowycz B, Plotnikova O, Farrelly E, Xiao SH, Chen G, Wang Z.
Bioorg Med Chem Lett (2013) 23 : 1238 -1244
PubMed 23374866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 5.97 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2334589 1 7.40
CHEMBL2334586 1 7.39
CHEMBL2334970 1 7.20
CHEMBL2334966 1 7.20
CHEMBL2334579 1 7.16
CHEMBL2334964 1 7.12
CHEMBL2334965 1 7.05
CHEMBL2334583 1 7.00
CHEMBL2334577 1 6.96
CHEMBL2334963 1 6.82
CHEMBL2334591 1 6.72
CHEMBL2334962 1 6.52
CHEMBL2334593 1 6.51
CHEMBL2334967 1 6.26
CHEMBL2334590 1 6.22
CHEMBL2334581 1 5.92
CHEMBL2334968 1 5.75
CHEMBL2334580 1 5.58
CHEMBL2334592 1 5.40
CHEMBL2334588 1 4.82
CHEMBL2334582 1 4.68
CHEMBL2334969 1 4.62
CHEMBL2334587 1 4.62
CHEMBL2334578 1 4.52
CHEMBL2334584 1 4.52
CHEMBL2334585 1 4.52
CHEMBL48082 1 4.39
CHEMBL2334971 1 4.38
CHEMBL2334575 1 -
CHEMBL2334576 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2334589 IC50 = 40.0 nM 7.40
CHEMBL2334586 IC50 = 41.0 nM 7.39
CHEMBL2334970 IC50 = 63.0 nM 7.20
CHEMBL2334966 IC50 = 63.0 nM 7.20
CHEMBL2334579 IC50 = 70.0 nM 7.16
CHEMBL2334964 IC50 = 76.0 nM 7.12
CHEMBL2334965 IC50 = 89.0 nM 7.05
CHEMBL2334583 IC50 = 100.0 nM 7.00
CHEMBL2334577 IC50 = 110.0 nM 6.96
CHEMBL2334963 IC50 = 150.0 nM 6.82
CHEMBL2334591 IC50 = 190.0 nM 6.72
CHEMBL2334962 IC50 = 300.0 nM 6.52
CHEMBL2334593 IC50 = 310.0 nM 6.51
CHEMBL2334967 IC50 = 550.0 nM 6.26
CHEMBL2334590 IC50 = 600.0 nM 6.22
CHEMBL2334581 IC50 = 1200.0 nM 5.92
CHEMBL2334968 IC50 = 1800.0 nM 5.75
CHEMBL2334580 IC50 = 2600.0 nM 5.58
CHEMBL2334592 IC50 = 4000.0 nM 5.40
CHEMBL2334588 IC50 = 15000.0 nM 4.82
CHEMBL2334582 IC50 = 21000.0 nM 4.68
CHEMBL2334969 IC50 = 24000.0 nM 4.62
CHEMBL2334587 IC50 = 24000.0 nM 4.62
CHEMBL2334578 IC50 = 30000.0 nM 4.52
CHEMBL2334584 IC50 = 30000.0 nM 4.52
CHEMBL2334585 IC50 = 30000.0 nM 4.52
CHEMBL48082 IC50 = 41000.0 nM 4.39
CHEMBL2334971 IC50 = 42000.0 nM 4.38
CHEMBL2334575 IC50 > 80000.0 nM -
CHEMBL2334576 IC50 > 80000.0 nM -
CHEMBL100979 IC50 > 80000.0 nM -