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Assay Detail

CHEMBL4835172

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Binding
Inhibition of human recombinant ADAMTS-5 assessed as cleavage of fluorescent substrate using FAM-TBIS-1 by biochemical assay
ChEMBL ↗
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

A disintegrin and metalloproteinase with thrombospondin motifs 5 (CHEMBL2285) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.
Brebion F, Gosmini R, Deprez P, Varin M, Peixoto C, Alvey L, Jary H, Bienvenu N, Triballeau N, Blanque R, Cottereaux C, Christophe T, Vandervoort N, Mollat P, Touitou R, Leonard P, De Ceuninck F, Botez I, Monjardet A, van der Aar E, Amantini D.
J Med Chem (2021) 64 : 2937 -2952
PubMed 33719441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 6.77 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4874034 — — 1 7.92
CHEMBL4846457 — — 1 7.75
CHEMBL4650334 ALDUMASTAT 2.0 1 7.72
CHEMBL4856943 — — 1 7.66
CHEMBL4868710 — — 1 7.66
CHEMBL4874226 — — 1 7.52
CHEMBL4872817 — — 1 7.50
CHEMBL4854306 — — 1 7.47
CHEMBL4854866 — — 1 7.47
CHEMBL4864100 — — 1 7.44
CHEMBL4877087 — — 1 7.39
CHEMBL4859812 — — 1 7.37
CHEMBL4863614 — — 1 7.34
CHEMBL4876618 — — 1 7.33
CHEMBL4862188 — — 1 7.32
CHEMBL4856883 — — 1 7.28
CHEMBL4877662 — — 1 7.26
CHEMBL4846698 — — 1 7.15
CHEMBL4850150 — — 1 7.08
CHEMBL4856230 — — 1 6.96
CHEMBL4872381 — — 1 6.91
CHEMBL4849855 — — 1 6.91
CHEMBL4856188 — — 1 6.81
CHEMBL4876864 — — 1 6.79
CHEMBL4873384 — — 1 6.76
CHEMBL4863647 — — 1 6.75
CHEMBL4870697 — — 1 6.64
CHEMBL4867911 — — 1 6.61
CHEMBL4870479 — — 1 6.60
CHEMBL4878543 — — 1 6.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4874034 — IC50 = 12.0 nM 7.92
CHEMBL4846457 — IC50 = 18.0 nM 7.75
CHEMBL4650334 ALDUMASTAT IC50 = 19.0 nM 7.72
CHEMBL4856943 — IC50 = 22.0 nM 7.66
CHEMBL4868710 — IC50 = 22.0 nM 7.66
CHEMBL4874226 — IC50 = 30.0 nM 7.52
CHEMBL4872817 — IC50 = 32.0 nM 7.50
CHEMBL4854306 — IC50 = 34.0 nM 7.47
CHEMBL4854866 — IC50 = 34.0 nM 7.47
CHEMBL4864100 — IC50 = 36.0 nM 7.44
CHEMBL4877087 — IC50 = 41.0 nM 7.39
CHEMBL4859812 — IC50 = 43.0 nM 7.37
CHEMBL4863614 — IC50 = 46.0 nM 7.34
CHEMBL4876618 — IC50 = 47.0 nM 7.33
CHEMBL4862188 — IC50 = 48.0 nM 7.32
CHEMBL4856883 — IC50 = 52.0 nM 7.28
CHEMBL4877662 — IC50 = 55.0 nM 7.26
CHEMBL4846698 — IC50 = 71.0 nM 7.15
CHEMBL4850150 — IC50 = 84.0 nM 7.08
CHEMBL4856230 — IC50 = 109.0 nM 6.96
CHEMBL4872381 — IC50 = 124.0 nM 6.91
CHEMBL4849855 — IC50 = 123.0 nM 6.91
CHEMBL4856188 — IC50 = 156.0 nM 6.81
CHEMBL4876864 — IC50 = 164.0 nM 6.79
CHEMBL4873384 — IC50 = 173.0 nM 6.76
CHEMBL4863647 — IC50 = 178.0 nM 6.75
CHEMBL4870697 — IC50 = 230.0 nM 6.64
CHEMBL4867911 — IC50 = 247.0 nM 6.61
CHEMBL4870479 — IC50 = 251.0 nM 6.60
CHEMBL4878543 — IC50 = 287.0 nM 6.54
CHEMBL4868229 — IC50 = 536.0 nM 6.27
CHEMBL4876898 — IC50 = 536.0 nM 6.27
CHEMBL4856611 — IC50 = 638.0 nM 6.20
CHEMBL4872734 — IC50 = 667.0 nM 6.18
CHEMBL4859417 — IC50 = 826.0 nM 6.08
CHEMBL4851316 — IC50 = 903.0 nM 6.04
CHEMBL4859727 — IC50 = 1045.0 nM 5.98
CHEMBL4866654 — IC50 = 1170.0 nM 5.93
CHEMBL4871605 — IC50 = 1232.0 nM 5.91
CHEMBL4850670 — IC50 = 1530.0 nM 5.82
CHEMBL4871267 — IC50 = 1749.0 nM 5.76
CHEMBL4863949 — IC50 = 2233.0 nM 5.65
CHEMBL4845900 — IC50 = 2469.0 nM 5.61
CHEMBL4870053 — IC50 = 2927.0 nM 5.53
CHEMBL4875821 — IC50 = 3388.0 nM 5.47
CHEMBL4857548 — IC50 > 4000.0 nM -
CHEMBL4871238 — IC50 > 20000.0 nM -
CHEMBL4877210 — IC50 > 20000.0 nM -
CHEMBL4846853 — IC50 > 4000.0 nM -
CHEMBL4863715 — IC50 > 20000.0 nM -