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Assay Detail

CHEMBL715849

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro inhibition of human Matrix metalloprotease-2.
21
Total Activities
21
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

Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.
Curtin ML, Florjancic AS, Heyman HR, Michaelides MR, Garland RB, Holms JH, Steinman DH, Dellaria JF, Gong J, Wada CK, Guo Y, Elmore IB, Tapang P, Albert DH, Magoc TJ, Marcotte PA, Bouska JJ, Goodfellow CL, Bauch JL, Marsh KC, Morgan DW, Davidsen SK.
Bioorg Med Chem Lett (2001) 11 : 1557 -1560
PubMed 11412980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.64 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL40151 1 9.00
CHEMBL416421 1 8.40
CHEMBL41408 1 8.40
CHEMBL40143 1 8.40
CHEMBL38868 1 8.40
CHEMBL43411 1 8.22
CHEMBL41102 1 8.10
CHEMBL42970 1 7.80
CHEMBL39566 1 7.70
CHEMBL41324 1 7.70
CHEMBL39601 1 7.58
CHEMBL285296 1 7.32
CHEMBL288067 1 7.24
CHEMBL38299 1 7.21
CHEMBL40613 1 7.07
CHEMBL288385 1 7.05
CHEMBL40335 1 6.89
CHEMBL41943 1 6.75
CHEMBL39921 1 5.89
CHEMBL418437 1 -
CHEMBL41150 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL40151 IC50 = 1.0 nM 9.00
CHEMBL416421 IC50 = 4.0 nM 8.40
CHEMBL41408 IC50 = 4.0 nM 8.40
CHEMBL40143 IC50 = 4.0 nM 8.40
CHEMBL38868 IC50 = 4.0 nM 8.40
CHEMBL43411 IC50 = 6.0 nM 8.22
CHEMBL41102 IC50 = 8.0 nM 8.10
CHEMBL42970 IC50 = 16.0 nM 7.80
CHEMBL39566 IC50 = 20.0 nM 7.70
CHEMBL41324 IC50 = 20.0 nM 7.70
CHEMBL39601 IC50 = 26.0 nM 7.58
CHEMBL285296 IC50 = 48.0 nM 7.32
CHEMBL288067 IC50 = 58.0 nM 7.24
CHEMBL38299 IC50 = 61.0 nM 7.21
CHEMBL40613 IC50 = 85.0 nM 7.07
CHEMBL288385 IC50 = 89.0 nM 7.05
CHEMBL40335 IC50 = 130.0 nM 6.89
CHEMBL41943 IC50 = 180.0 nM 6.75
CHEMBL39921 IC50 = 1300.0 nM 5.89
CHEMBL418437 IC50 > 10000.0 nM -
CHEMBL41150 IC50 > 10000.0 nM -