Assay Detail
Binding
CHEMBL1806085
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Inhibition of human MMP3 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay
29
Total Activities
29
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 |
Publication
Orally active MMP-1 sparing α-tetrahydropyranyl and α-piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.63 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1801056 | — | — | 1 | 9.70 |
| CHEMBL1801044 | — | — | 1 | 8.15 |
| CHEMBL1082381 | — | — | 1 | 7.89 |
| CHEMBL1801420 | — | — | 1 | 7.74 |
| CHEMBL1801045 | — | — | 1 | 7.74 |
| CHEMBL1801046 | — | — | 1 | 7.74 |
| CHEMBL1801396 | — | — | 1 | 7.74 |
| CHEMBL1801054 | — | — | 1 | 7.70 |
| CHEMBL1801421 | — | — | 1 | 7.70 |
| CHEMBL1801057 | — | — | 1 | 7.69 |
| CHEMBL1801429 | — | — | 1 | 7.67 |
| CHEMBL1801423 | — | — | 1 | 7.67 |
| CHEMBL1229868 | — | — | 1 | 7.66 |
| CHEMBL1801430 | — | — | 1 | 7.66 |
| CHEMBL1801415 | — | — | 1 | 7.65 |
| CHEMBL1801428 | — | — | 1 | 7.62 |
| CHEMBL1771212 | — | — | 1 | 7.54 |
| CHEMBL1801413 | — | — | 1 | 7.49 |
| CHEMBL1801419 | — | — | 1 | 7.46 |
| CHEMBL1801052 | — | — | 1 | 7.46 |
| CHEMBL1801047 | — | — | 1 | 7.46 |
| CHEMBL1801427 | — | — | 1 | 7.43 |
| CHEMBL1801426 | — | — | 1 | 7.40 |
| CHEMBL1801393 | — | — | 1 | 7.37 |
| CHEMBL1801050 | — | — | 1 | 7.30 |
| CHEMBL1801051 | — | — | 1 | 7.26 |
| CHEMBL1801425 | — | — | 1 | 7.19 |
| CHEMBL1801424 | — | — | 1 | 7.12 |
| CHEMBL1801431 | — | — | 1 | 6.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1801056 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1801044 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1082381 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1801420 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL1801045 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL1801046 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL1801396 | — | IC50 | = | 18.1 | nM | 7.74 |
| CHEMBL1801054 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1801421 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1801057 | — | IC50 | = | 20.6 | nM | 7.69 |
| CHEMBL1801429 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL1801423 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL1229868 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1801430 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1801415 | — | IC50 | = | 22.5 | nM | 7.65 |
| CHEMBL1801428 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL1771212 | — | IC50 | = | 28.7 | nM | 7.54 |
| CHEMBL1801413 | — | IC50 | = | 32.6 | nM | 7.49 |
| CHEMBL1801419 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1801052 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1801047 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1801427 | — | IC50 | = | 36.9 | nM | 7.43 |
| CHEMBL1801426 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1801393 | — | IC50 | = | 42.5 | nM | 7.37 |
| CHEMBL1801050 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1801051 | — | IC50 | = | 55.3 | nM | 7.26 |
| CHEMBL1801425 | — | IC50 | = | 64.7 | nM | 7.19 |
| CHEMBL1801424 | — | IC50 | = | 76.8 | nM | 7.12 |
| CHEMBL1801431 | — | IC50 | = | 115.0 | nM | 6.94 |