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Assay Detail

CHEMBL1292818

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Binding
Inhibition of TACE
ChEMBL ↗
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Disintegrin and metalloproteinase domain-containing protein 17 (CHEMBL3706) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases.
Girijavallabhan VM, Chen L, Dai C, Feltz RJ, Firmansjah L, Li D, Kim SH, Kozlowski JA, Lavey BJ, Kosinski A, Piwinski JJ, Popovici-Muller J, Rizvi R, Rosner KE, Shankar BB, Shih NY, Siddiqui MA, Tong L, Wong MK, Yang DY, Yang L, Yu W, Zhou G, Guo Z, Orth P, Madison V, Bian H, Lundell D, Niu X, Shah H, Sun J, Umland S.
Bioorg Med Chem Lett (2010) 20 : 7283 -7287
PubMed 21106451 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 9.42 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1288122 — — 1 10.22
CHEMBL1288000 — — 1 10.15
CHEMBL1288726 — — 1 10.00
CHEMBL1288059 — — 1 9.89
CHEMBL1287998 — — 1 9.85
CHEMBL1287939 — — 1 9.80
CHEMBL1287909 — — 1 9.80
CHEMBL1288241 — — 1 9.77
CHEMBL1287969 — — 1 9.74
CHEMBL1288267 — — 1 9.72
CHEMBL1288029 — — 1 9.70
CHEMBL1287999 — — 1 9.66
CHEMBL1288028 — — 1 9.59
CHEMBL1287881 — — 1 9.54
CHEMBL1288060 — — 1 9.39
CHEMBL1288211 — — 1 9.38
CHEMBL1287908 — — 1 9.33
CHEMBL1288212 — — 1 9.30
CHEMBL1288090 — — 1 9.30
CHEMBL1288296 — — 1 9.28
CHEMBL1288268 — — 1 9.28
CHEMBL1288152 — — 1 9.25
CHEMBL1288295 — — 1 9.22
CHEMBL1287851 — — 1 9.21
CHEMBL1287882 — — 1 9.21
CHEMBL1288091 — — 1 9.14
CHEMBL1288151 — — 1 9.07
CHEMBL1287852 — — 1 9.04
CHEMBL1288121 — — 1 8.70
CHEMBL1288240 — — 1 8.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1288122 — Ki = 0.06 nM 10.22
CHEMBL1288000 — Ki = 0.07 nM 10.15
CHEMBL1288726 — Ki = 0.1 nM 10.00
CHEMBL1288059 — Ki = 0.13 nM 9.89
CHEMBL1287998 — Ki = 0.14 nM 9.85
CHEMBL1287939 — Ki = 0.16 nM 9.80
CHEMBL1287909 — Ki = 0.16 nM 9.80
CHEMBL1288241 — Ki = 0.17 nM 9.77
CHEMBL1287969 — Ki = 0.18 nM 9.74
CHEMBL1288267 — Ki = 0.19 nM 9.72
CHEMBL1288029 — Ki = 0.2 nM 9.70
CHEMBL1287999 — Ki = 0.22 nM 9.66
CHEMBL1288028 — Ki = 0.26 nM 9.59
CHEMBL1287881 — Ki = 0.29 nM 9.54
CHEMBL1288060 — Ki = 0.41 nM 9.39
CHEMBL1288211 — Ki = 0.42 nM 9.38
CHEMBL1287908 — Ki = 0.47 nM 9.33
CHEMBL1288212 — Ki = 0.5 nM 9.30
CHEMBL1288090 — Ki = 0.5 nM 9.30
CHEMBL1288296 — Ki = 0.53 nM 9.28
CHEMBL1288268 — Ki = 0.52 nM 9.28
CHEMBL1288152 — Ki = 0.56 nM 9.25
CHEMBL1288295 — Ki = 0.6 nM 9.22
CHEMBL1287851 — Ki = 0.62 nM 9.21
CHEMBL1287882 — Ki = 0.61 nM 9.21
CHEMBL1288091 — Ki = 0.72 nM 9.14
CHEMBL1288151 — Ki = 0.85 nM 9.07
CHEMBL1287852 — Ki = 0.92 nM 9.04
CHEMBL1288121 — Ki = 2.0 nM 8.70
CHEMBL1288240 — Ki = 2.35 nM 8.63
CHEMBL1288183 — Ki = 2.55 nM 8.59
CHEMBL1288182 — Ki = 2.78 nM 8.56