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Assay Detail

CHEMBL1775258

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

Binding
Inhibition of IKK2 using 5-FAM-GRHDSGLDSMK-NH2 as substrate by TR-FRET assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Discovery of piperidinyl aminopyrimidine derivatives as IKK-2 inhibitors.
Kim S, Jung JK, Lee HS, Kim Y, Kim J, Choi K, Baek DJ, Moon B, Oh KS, Lee BH, Shin KJ, Pae AN, Nam G, Roh EJ, Cho YS, Choo H.
Bioorg Med Chem Lett (2011) 21 : 3002 -3006
PubMed 21489792 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.56 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360077 1 6.82
CHEMBL1773329 1 6.04
CHEMBL1773334 1 5.89
CHEMBL1773327 1 5.68
CHEMBL1773328 1 5.66
CHEMBL1775219 1 5.50
CHEMBL1773335 1 5.50
CHEMBL1775231 1 5.43
CHEMBL1773336 1 5.42
CHEMBL1775233 1 5.42
CHEMBL1773333 1 5.37
CHEMBL1773330 1 5.25
CHEMBL1773331 1 5.15
CHEMBL1773326 1 4.71
CHEMBL1775224 1 -
CHEMBL1775225 1 -
CHEMBL1775226 1 -
CHEMBL1775227 1 -
CHEMBL1775228 1 -
CHEMBL1775229 1 -
CHEMBL1775230 1 -
CHEMBL1775232 1 -
CHEMBL1775234 1 -
CHEMBL1775235 1 -
CHEMBL1775237 1 -
CHEMBL1775238 1 -
CHEMBL1775236 1 -
CHEMBL1775239 1 -
CHEMBL1773325 1 -
CHEMBL1773332 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360077 IC50 = 150.0 nM 6.82
CHEMBL1773329 IC50 = 920.0 nM 6.04
CHEMBL1773334 IC50 = 1300.0 nM 5.89
CHEMBL1773327 IC50 = 2090.0 nM 5.68
CHEMBL1773328 IC50 = 2200.0 nM 5.66
CHEMBL1775219 IC50 = 3200.0 nM 5.50
CHEMBL1773335 IC50 = 3140.0 nM 5.50
CHEMBL1775231 IC50 = 3670.0 nM 5.43
CHEMBL1773336 IC50 = 3850.0 nM 5.42
CHEMBL1775233 IC50 = 3800.0 nM 5.42
CHEMBL1773333 IC50 = 4250.0 nM 5.37
CHEMBL1773330 IC50 = 5600.0 nM 5.25
CHEMBL1773331 IC50 = 7020.0 nM 5.15
CHEMBL1773326 IC50 = 19700.0 nM 4.71
CHEMBL1775220 IC50 - -
CHEMBL1775221 IC50 - -
CHEMBL1775222 IC50 - -
CHEMBL1775223 IC50 - -
CHEMBL1775224 IC50 - -
CHEMBL1775225 IC50 - -
CHEMBL1775226 IC50 - -
CHEMBL1775227 IC50 - -
CHEMBL1775228 IC50 - -
CHEMBL1775229 IC50 - -
CHEMBL1775230 IC50 - -
CHEMBL1775232 IC50 - -
CHEMBL1775234 IC50 - -
CHEMBL1775235 IC50 - -
CHEMBL1775237 IC50 - -
CHEMBL1775238 IC50 - -
CHEMBL1775236 IC50 - -
CHEMBL1775239 IC50 - -
CHEMBL1773325 IC50 - -
CHEMBL1773332 IC50 - -