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Assay Detail

CHEMBL1002944

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Binding
Inhibition of MMP2
40
Total Activities
40
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge.
Georgiadis D, Yiotakis A.
Bioorg Med Chem (2008) 16 : 8781 -8794
PubMed 18790648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.52 7.86
IC50 18 6.41 8.40
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40143 1 8.40
CHEMBL181244 1 7.92
CHEMBL483857 1 7.86
CHEMBL445971 1 7.80
CHEMBL447457 1 7.52
CHEMBL434567 1 7.46
CHEMBL520785 1 7.34
CHEMBL485492 1 6.96
CHEMBL497772 1 6.87
CHEMBL507420 1 6.72
CHEMBL209970 1 6.45
CHEMBL251917 1 6.28
CHEMBL484262 1 6.18
CHEMBL503231 1 6.12
CHEMBL98044 1 6.05
CHEMBL399096 1 6.02
CHEMBL402747 1 5.89
CHEMBL117225 1 5.75
CHEMBL148169 1 5.69
CHEMBL395880 1 5.66
CHEMBL270083 1 5.40
CHEMBL24398 1 5.20
CHEMBL50228 1 5.09
CHEMBL250266 1 4.47
CHEMBL389020 1 -
CHEMBL508461 1 -
CHEMBL523956 1 -
CHEMBL491643 1 -
CHEMBL497985 1 -
CHEMBL318252 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40143 IC50 = 4.0 nM 8.40
CHEMBL181244 IC50 = 12.0 nM 7.92
CHEMBL483857 Ki = 13.9 nM 7.86
CHEMBL445971 Ki = 16.0 nM 7.80
CHEMBL447457 Ki = 30.0 nM 7.52
CHEMBL434567 IC50 = 35.0 nM 7.46
CHEMBL520785 Ki = 46.0 nM 7.34
CHEMBL485492 Ki = 110.0 nM 6.96
CHEMBL497772 IC50 = 135.0 nM 6.87
CHEMBL507420 Ki = 192.0 nM 6.72
CHEMBL209970 IC50 = 355.0 nM 6.45
CHEMBL251917 IC50 = 529.0 nM 6.28
CHEMBL484262 IC50 = 664.0 nM 6.18
CHEMBL503231 IC50 = 750.0 nM 6.12
CHEMBL98044 IC50 = 900.0 nM 6.05
CHEMBL399096 IC50 = 960.0 nM 6.02
CHEMBL402747 Ki = 1300.0 nM 5.89
CHEMBL117225 IC50 = 1790.0 nM 5.75
CHEMBL148169 Ki = 2050.0 nM 5.69
CHEMBL395880 Ki = 2170.0 nM 5.66
CHEMBL270083 IC50 = 4000.0 nM 5.40
CHEMBL24398 Ki = 6300.0 nM 5.20
CHEMBL50228 Ki = 8100.0 nM 5.09
CHEMBL250266 IC50 = 34200.0 nM 4.47
CHEMBL270050 Activity - -
CHEMBL325163 Ki > 2000.0 nM -
CHEMBL108494 Ki > 15000.0 nM -
CHEMBL489603 IC50 > 50000.0 nM -
CHEMBL496527 Ki > 3333.0 nM -
CHEMBL207305 Ki > 3333.0 nM -
CHEMBL495502 Ki > 3000.0 nM -
CHEMBL253275 Ki > 10000.0 nM -
CHEMBL402393 Ki > 3333.0 nM -
CHEMBL228320 Ki > 3333.0 nM -
CHEMBL318252 IC50 > 100000.0 nM -
CHEMBL497985 IC50 > 5000.0 nM -
CHEMBL491643 IC50 > 5000.0 nM -
CHEMBL523956 Ki > 3000.0 nM -
CHEMBL508461 IC50 > 100000.0 nM -
CHEMBL389020 Ki > 100000.0 nM -