Assay Detail
Binding
CHEMBL1806090
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Inhibition of human MMP14 assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay
40
Total Activities
40
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 | 40 | 7.72 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1801422 | — | — | 1 | 9.14 |
| CHEMBL1801397 | — | — | 1 | 8.88 |
| CHEMBL1801048 | — | — | 1 | 8.77 |
| CHEMBL1801057 | — | — | 1 | 8.51 |
| CHEMBL1801053 | — | — | 1 | 8.44 |
| CHEMBL1801393 | — | — | 1 | 8.43 |
| CHEMBL1801421 | — | — | 1 | 8.40 |
| CHEMBL1801431 | — | — | 1 | 8.39 |
| CHEMBL1801045 | — | — | 1 | 8.35 |
| CHEMBL1801430 | — | — | 1 | 8.34 |
| CHEMBL1801046 | — | — | 1 | 8.25 |
| CHEMBL1801412 | — | — | 1 | 8.17 |
| CHEMBL1801399 | — | — | 1 | 8.15 |
| CHEMBL1800089 | — | — | 1 | 8.13 |
| CHEMBL1801396 | — | — | 1 | 8.05 |
| CHEMBL1801394 | — | — | 1 | 8.02 |
| CHEMBL1801049 | — | — | 1 | 7.98 |
| CHEMBL1801052 | — | — | 1 | 7.97 |
| CHEMBL1771212 | — | — | 1 | 7.89 |
| CHEMBL1801417 | — | — | 1 | 7.88 |
| CHEMBL1801420 | — | — | 1 | 7.83 |
| CHEMBL1082381 | — | — | 1 | 7.72 |
| CHEMBL1801050 | — | — | 1 | 7.70 |
| CHEMBL1801051 | — | — | 1 | 7.62 |
| CHEMBL1801398 | — | — | 1 | 7.60 |
| CHEMBL1801416 | — | — | 1 | 7.59 |
| CHEMBL1801047 | — | — | 1 | 7.33 |
| CHEMBL1801423 | — | — | 1 | 7.31 |
| CHEMBL1801413 | — | — | 1 | 7.27 |
| CHEMBL1801429 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1801422 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL1801397 | — | IC50 | = | 1.33 | nM | 8.88 |
| CHEMBL1801048 | — | IC50 | = | 1.71 | nM | 8.77 |
| CHEMBL1801057 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL1801053 | — | IC50 | = | 3.63 | nM | 8.44 |
| CHEMBL1801393 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1801421 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1801431 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1801045 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1801430 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL1801046 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL1801412 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL1801399 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL1800089 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1801396 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1801394 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL1801049 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL1801052 | — | IC50 | = | 10.6 | nM | 7.97 |
| CHEMBL1771212 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1801417 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL1801420 | — | IC50 | = | 14.9 | nM | 7.83 |
| CHEMBL1082381 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL1801050 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1801051 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1801398 | — | IC50 | = | 24.9 | nM | 7.60 |
| CHEMBL1801416 | — | IC50 | = | 25.8 | nM | 7.59 |
| CHEMBL1801047 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1801423 | — | IC50 | = | 49.4 | nM | 7.31 |
| CHEMBL1801413 | — | IC50 | = | 53.9 | nM | 7.27 |
| CHEMBL1801429 | — | IC50 | = | 53.3 | nM | 7.27 |
| CHEMBL1801426 | — | IC50 | = | 58.6 | nM | 7.23 |
| CHEMBL1229868 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1801419 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL1801427 | — | IC50 | = | 100.5 | nM | 7.00 |
| CHEMBL1801428 | — | IC50 | = | 108.0 | nM | 6.97 |
| CHEMBL1801425 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1801415 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL1801054 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1801424 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1801418 | — | IC50 | = | 3486.0 | nM | 5.46 |