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Assay Detail

CHEMBL1764206

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Binding
Inhibition of IKK-alpha
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-β.
Miller DD, Bamborough P, Christopher JA, Baldwin IR, Champigny AC, Cutler GJ, Kerns JK, Longstaff T, Mellor GW, Morey JV, Morse MA, Nie H, Rumsey WL, Taggart JJ.
Bioorg Med Chem Lett (2011) 21 : 2255 -2258
PubMed 21429745 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.21 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1761510 1 5.80
CHEMBL1761514 1 5.70
CHEMBL1761512 1 5.70
CHEMBL1761513 1 5.50
CHEMBL1761501 1 5.40
CHEMBL1761509 1 5.40
CHEMBL1761503 1 5.30
CHEMBL1761504 1 5.20
CHEMBL1761515 1 5.10
CHEMBL1761500 1 5.00
CHEMBL1761511 1 5.00
CHEMBL1761499 1 5.00
CHEMBL1761508 1 4.90
CHEMBL1964241 1 4.80
CHEMBL1761506 1 4.80
CHEMBL1761505 1 4.80
CHEMBL1761502 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1761510 IC50 = 1584.89 nM 5.80
CHEMBL1761514 IC50 = 1995.26 nM 5.70
CHEMBL1761512 IC50 = 1995.26 nM 5.70
CHEMBL1761513 IC50 = 3162.28 nM 5.50
CHEMBL1761501 IC50 = 3981.07 nM 5.40
CHEMBL1761509 IC50 = 3981.07 nM 5.40
CHEMBL1761503 IC50 = 5011.87 nM 5.30
CHEMBL1761504 IC50 = 6309.57 nM 5.20
CHEMBL1761515 IC50 = 7943.28 nM 5.10
CHEMBL1761500 IC50 = 10000.0 nM 5.00
CHEMBL1761511 IC50 = 10000.0 nM 5.00
CHEMBL1761499 IC50 = 10000.0 nM 5.00
CHEMBL1761508 IC50 = 12589.25 nM 4.90
CHEMBL1964241 IC50 = 15848.93 nM 4.80
CHEMBL1761506 IC50 = 15848.93 nM 4.80
CHEMBL1761505 IC50 = 15848.93 nM 4.80
CHEMBL1761502 IC50 > 15848.93 nM -