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Assay Detail

CHEMBL718937

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Binding
In vitro selective inhibition against matrix metalloprotease-2 (MMP-2) using fluorimetric assay
ChEMBL ↗
47
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

72 kDa type IV collagenase (CHEMBL333) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.
Wada CK, Holms JH, Curtin ML, Dai Y, Florjancic AS, Garland RB, Guo Y, Heyman HR, Stacey JR, Steinman DH, Albert DH, Bouska JJ, Elmore IN, Goodfellow CL, Marcotte PA, Tapang P, Morgan DW, Michaelides MR, Davidsen SK.
J Med Chem (2002) 45 : 219 -232
PubMed 11754593 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 8.77 10.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75094 PRINOMASTAT 3.0 1 10.32
CHEMBL311141 — — 1 10.01
CHEMBL75302 — — 1 9.49
CHEMBL78052 — — 1 9.48
CHEMBL308264 — — 1 9.47
CHEMBL307413 — — 1 9.46
CHEMBL75487 — — 1 9.46
CHEMBL75164 — — 1 9.44
CHEMBL75529 — — 1 9.41
CHEMBL279785 MARIMASTAT 3.0 1 9.39
CHEMBL306276 — — 1 9.38
CHEMBL309329 — — 1 9.36
CHEMBL75154 — — 1 9.35
CHEMBL78145 — — 1 9.28
CHEMBL75189 — — 1 9.24
CHEMBL75114 — — 1 9.21
CHEMBL76757 — — 1 9.17
CHEMBL75139 — — 1 9.14
CHEMBL2115165 — — 2 9.11
CHEMBL76043 — — 1 9.07
CHEMBL307372 — — 1 9.04
CHEMBL311618 — — 1 9.03
CHEMBL309053 — — 1 8.89
CHEMBL75567 — — 1 8.89
CHEMBL73652 — — 1 8.85
CHEMBL306301 — — 1 8.82
CHEMBL73928 — — 1 8.77
CHEMBL77907 — — 1 8.74
CHEMBL3037894 — — 1 8.72
CHEMBL306050 — — 1 8.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75094 PRINOMASTAT IC50 = 0.048 nM 10.32
CHEMBL311141 — IC50 = 0.098 nM 10.01
CHEMBL75302 — IC50 = 0.32 nM 9.49
CHEMBL78052 — IC50 = 0.33 nM 9.48
CHEMBL308264 — IC50 = 0.34 nM 9.47
CHEMBL75487 — IC50 = 0.35 nM 9.46
CHEMBL307413 — IC50 = 0.35 nM 9.46
CHEMBL75164 — IC50 = 0.36 nM 9.44
CHEMBL75529 — IC50 = 0.39 nM 9.41
CHEMBL279785 MARIMASTAT IC50 = 0.41 nM 9.39
CHEMBL306276 — IC50 = 0.42 nM 9.38
CHEMBL309329 — IC50 = 0.44 nM 9.36
CHEMBL75154 — IC50 = 0.45 nM 9.35
CHEMBL78145 — IC50 = 0.53 nM 9.28
CHEMBL75189 — IC50 = 0.57 nM 9.24
CHEMBL75114 — IC50 = 0.61 nM 9.21
CHEMBL76757 — IC50 = 0.67 nM 9.17
CHEMBL75139 — IC50 = 0.72 nM 9.14
CHEMBL2115165 — IC50 = 0.78 nM 9.11
CHEMBL76043 — IC50 = 0.86 nM 9.07
CHEMBL307372 — IC50 = 0.91 nM 9.04
CHEMBL311618 — IC50 = 0.93 nM 9.03
CHEMBL309053 — IC50 = 1.3 nM 8.89
CHEMBL75567 — IC50 = 1.3 nM 8.89
CHEMBL73652 — IC50 = 1.4 nM 8.85
CHEMBL306301 — IC50 = 1.5 nM 8.82
CHEMBL73928 — IC50 = 1.7 nM 8.77
CHEMBL77907 — IC50 = 1.8 nM 8.74
CHEMBL3037894 — IC50 = 1.9 nM 8.72
CHEMBL306050 — IC50 = 1.9 nM 8.72
CHEMBL73866 — IC50 = 2.4 nM 8.62
CHEMBL75618 — IC50 = 2.4 nM 8.62
CHEMBL306585 — IC50 = 2.6 nM 8.59
CHEMBL77874 — IC50 = 2.8 nM 8.55
CHEMBL74151 — IC50 = 3.6 nM 8.44
CHEMBL75437 — IC50 = 3.7 nM 8.43
CHEMBL2114138 — IC50 = 6.3 nM 8.20
CHEMBL307915 — IC50 = 7.4 nM 8.13
CHEMBL74812 — IC50 = 9.5 nM 8.02
CHEMBL261932 TANOMASTAT IC50 = 11.0 nM 7.96
CHEMBL275654 — IC50 = 12.0 nM 7.92
CHEMBL75464 — IC50 = 20.0 nM 7.70
CHEMBL2115165 — IC50 = 25.0 nM 7.60
CHEMBL78213 — IC50 = 34.0 nM 7.47
CHEMBL76222 REBIMASTAT IC50 = 41.0 nM 7.39
CHEMBL74365 — IC50 = 62.0 nM 7.21
CHEMBL2114138 — IC50 = 260.0 nM 6.58