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Assay Detail

CHEMBL899676

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Binding
Inhibition of ADAMTS5 by FRET assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

5'-Phenyl-3'H-spiro[indoline-3,2'-[1,3,4]thiadiazol]-2-one inhibitors of ADAMTS-5 (aggrecanase-2).
Bursavich MG, Gilbert AM, Lombardi S, Georgiadis KE, Reifenberg E, Flannery CR, Morris EA.
Bioorg Med Chem Lett (2007) 17 : 5630 -5633
PubMed 17804234 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.55 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237148 1 6.21
CHEMBL401435 1 6.19
CHEMBL236523 1 6.11
CHEMBL237149 1 6.06
CHEMBL237366 1 6.05
CHEMBL237368 1 6.02
CHEMBL236942 1 5.92
CHEMBL236525 1 5.92
CHEMBL236105 1 5.85
CHEMBL236316 1 5.85
CHEMBL393651 1 5.85
CHEMBL237367 1 5.82
CHEMBL235891 1 5.72
CHEMBL236317 1 5.70
CHEMBL236318 1 5.62
CHEMBL392395 1 5.60
CHEMBL428379 1 5.58
CHEMBL391124 1 5.52
CHEMBL400202 1 5.51
CHEMBL235890 1 5.43
CHEMBL400201 1 5.36
CHEMBL444891 1 5.34
CHEMBL235889 1 5.14
CHEMBL236944 1 5.12
CHEMBL391123 1 5.02
CHEMBL394936 1 4.96
CHEMBL236106 1 4.87
CHEMBL238012 1 4.87
CHEMBL393652 1 4.62
CHEMBL438674 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237148 IC50 = 610.0 nM 6.21
CHEMBL401435 IC50 = 640.0 nM 6.19
CHEMBL236523 IC50 = 780.0 nM 6.11
CHEMBL237149 IC50 = 870.0 nM 6.06
CHEMBL237366 IC50 = 900.0 nM 6.05
CHEMBL237368 IC50 = 950.0 nM 6.02
CHEMBL236942 IC50 = 1200.0 nM 5.92
CHEMBL236525 IC50 = 1200.0 nM 5.92
CHEMBL236105 IC50 = 1400.0 nM 5.85
CHEMBL236316 IC50 = 1400.0 nM 5.85
CHEMBL393651 IC50 = 1400.0 nM 5.85
CHEMBL237367 IC50 = 1500.0 nM 5.82
CHEMBL235891 IC50 = 1900.0 nM 5.72
CHEMBL236317 IC50 = 2000.0 nM 5.70
CHEMBL236318 IC50 = 2400.0 nM 5.62
CHEMBL392395 IC50 = 2500.0 nM 5.60
CHEMBL428379 IC50 = 2600.0 nM 5.58
CHEMBL391124 IC50 = 3000.0 nM 5.52
CHEMBL400202 IC50 = 3100.0 nM 5.51
CHEMBL235890 IC50 = 3700.0 nM 5.43
CHEMBL400201 IC50 = 4400.0 nM 5.36
CHEMBL444891 IC50 = 4600.0 nM 5.34
CHEMBL235889 IC50 = 7200.0 nM 5.14
CHEMBL236944 IC50 = 7500.0 nM 5.12
CHEMBL391123 IC50 = 9600.0 nM 5.02
CHEMBL394936 IC50 = 11100.0 nM 4.96
CHEMBL236106 IC50 = 13400.0 nM 4.87
CHEMBL238012 IC50 = 13600.0 nM 4.87
CHEMBL393652 IC50 = 24100.0 nM 4.62
CHEMBL438674 IC50 = 24200.0 nM 4.62