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Assay Detail

CHEMBL2167031

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

Functional
Inhibition of LPS-stimulated TNFalpha production in human Whole blood
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Blood
Confidence 1 — Organism
Curated By Autocuration

Target

Blood (CHEMBL613416)
Type TISSUE
Organism Homo sapiens

Publication

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Liddle J, Bamborough P, Barker MD, Campos S, Chung CW, Cousins RP, Faulder P, Heathcote ML, Hobbs H, Holmes DS, Ioannou C, Ramirez-Molina C, Morse MA, Osborn R, Payne JJ, Pritchard JM, Rumsey WL, Tape DT, Vicentini G, Whitworth C, Williamson RA.
Bioorg Med Chem Lett (2012) 22 : 5222 -5226
PubMed 22801646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.03 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164412 1 6.60
CHEMBL2164411 1 6.60
CHEMBL483165 1 6.40
CHEMBL2164410 1 6.40
CHEMBL2164417 1 6.40
CHEMBL2164426 1 6.30
CHEMBL2164413 1 6.20
CHEMBL2164415 1 6.20
CHEMBL2164424 1 6.00
CHEMBL2164425 1 6.00
CHEMBL2164423 1 6.00
CHEMBL2164418 1 6.00
CHEMBL2164427 1 5.90
CHEMBL2164416 1 5.90
CHEMBL2164414 1 5.90
CHEMBL2164422 1 5.90
CHEMBL2164421 1 5.80
CHEMBL483557 1 5.60
CHEMBL2164420 1 5.60
CHEMBL2164419 1 5.50
CHEMBL520308 1 5.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164412 IC50 = 251.19 nM 6.60
CHEMBL2164411 IC50 = 251.19 nM 6.60
CHEMBL483165 IC50 = 398.11 nM 6.40
CHEMBL2164410 IC50 = 398.11 nM 6.40
CHEMBL2164417 IC50 = 398.11 nM 6.40
CHEMBL2164426 IC50 = 501.19 nM 6.30
CHEMBL2164413 IC50 = 630.96 nM 6.20
CHEMBL2164415 IC50 = 630.96 nM 6.20
CHEMBL2164424 IC50 = 1000.0 nM 6.00
CHEMBL2164425 IC50 = 1000.0 nM 6.00
CHEMBL2164423 IC50 = 1000.0 nM 6.00
CHEMBL2164418 IC50 = 1000.0 nM 6.00
CHEMBL2164427 IC50 = 1258.93 nM 5.90
CHEMBL2164416 IC50 = 1258.93 nM 5.90
CHEMBL2164414 IC50 = 1258.93 nM 5.90
CHEMBL2164422 IC50 = 1258.93 nM 5.90
CHEMBL2164421 IC50 = 1584.89 nM 5.80
CHEMBL483557 IC50 = 2511.89 nM 5.60
CHEMBL2164420 IC50 = 2511.89 nM 5.60
CHEMBL2164419 IC50 = 3162.28 nM 5.50
CHEMBL520308 IC50 = 3162.28 nM 5.50