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Assay Detail

CHEMBL921616

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Binding
Inhibition of IKK2
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Synthesis and structure-activity relationship of aminopyrimidine IKK2 inhibitors.
Bingham AH, Davenport RJ, Fosbeary R, Gowers L, Knight RL, Lowe C, Owen DA, Parry DM, Pitt WR.
Bioorg Med Chem Lett (2008) 18 : 3622 -3627
PubMed 18501602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.15 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129857 AS-602868 1.0 1 7.21
CHEMBL257805 1 7.19
CHEMBL254556 1 6.89
CHEMBL402041 1 6.64
CHEMBL257402 1 6.60
CHEMBL254793 1 6.57
CHEMBL257189 1 6.42
CHEMBL403615 1 6.40
CHEMBL256524 1 6.39
CHEMBL402628 1 6.39
CHEMBL256148 1 6.36
CHEMBL256523 1 6.27
CHEMBL401919 1 6.22
CHEMBL428424 1 6.16
CHEMBL256347 1 6.00
CHEMBL256940 1 5.82
CHEMBL255436 1 5.60
CHEMBL402314 1 5.44
CHEMBL256285 1 5.40
CHEMBL440404 1 5.18
CHEMBL257769 1 5.05
CHEMBL404688 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129857 AS-602868 IC50 = 62.0 nM 7.21
CHEMBL257805 IC50 = 64.0 nM 7.19
CHEMBL254556 IC50 = 130.0 nM 6.89
CHEMBL402041 IC50 = 230.0 nM 6.64
CHEMBL257402 IC50 = 250.0 nM 6.60
CHEMBL254793 IC50 = 270.0 nM 6.57
CHEMBL257189 IC50 = 380.0 nM 6.42
CHEMBL403615 IC50 = 400.0 nM 6.40
CHEMBL256524 IC50 = 410.0 nM 6.39
CHEMBL402628 IC50 = 410.0 nM 6.39
CHEMBL256148 IC50 = 440.0 nM 6.36
CHEMBL256523 IC50 = 540.0 nM 6.27
CHEMBL401919 IC50 = 600.0 nM 6.22
CHEMBL428424 IC50 = 700.0 nM 6.16
CHEMBL256347 IC50 = 990.0 nM 6.00
CHEMBL256940 IC50 = 1500.0 nM 5.82
CHEMBL255436 IC50 = 2500.0 nM 5.60
CHEMBL402314 IC50 = 3600.0 nM 5.44
CHEMBL256285 IC50 = 4000.0 nM 5.40
CHEMBL440404 IC50 = 6600.0 nM 5.18
CHEMBL257769 IC50 = 8900.0 nM 5.05
CHEMBL404688 IC50 = 8900.0 nM 5.05