Assay Detail
Binding
CHEMBL1806083
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Inhibition of human MMP1 expressed in human HT-1080 cells assessed as cleavage of fluorogenic peptide MCAPro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 by fluorometric assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HT-1080 |
| 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 | 45 | 5.60 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1801044 | — | — | 1 | 6.57 |
| CHEMBL1801049 | — | — | 1 | 6.52 |
| CHEMBL1801048 | — | — | 1 | 6.40 |
| CHEMBL1801046 | — | — | 1 | 6.36 |
| CHEMBL1801417 | — | — | 1 | 6.11 |
| CHEMBL1801422 | — | — | 1 | 6.00 |
| CHEMBL1801412 | — | — | 1 | 6.00 |
| CHEMBL1801052 | — | — | 1 | 5.94 |
| CHEMBL1801050 | — | — | 1 | 5.85 |
| CHEMBL1801045 | — | — | 1 | 5.75 |
| CHEMBL1801416 | — | — | 1 | 5.70 |
| CHEMBL1801420 | — | — | 1 | 5.70 |
| CHEMBL1801421 | — | — | 1 | 5.62 |
| CHEMBL1801053 | — | — | 1 | 5.60 |
| CHEMBL1801397 | — | — | 1 | 5.58 |
| CHEMBL1801047 | — | — | 1 | 5.44 |
| CHEMBL1801056 | — | — | 1 | 5.44 |
| CHEMBL1801396 | — | — | 1 | 5.44 |
| CHEMBL1801430 | — | — | 1 | 5.40 |
| CHEMBL1801419 | — | — | 1 | 5.36 |
| CHEMBL1801395 | — | — | 1 | 5.35 |
| CHEMBL1801057 | — | — | 1 | 5.35 |
| CHEMBL1801393 | — | — | 1 | 5.34 |
| CHEMBL1801055 | — | — | 1 | 5.30 |
| CHEMBL1801054 | — | — | 1 | 5.30 |
| CHEMBL1801394 | — | — | 1 | 5.23 |
| CHEMBL1801423 | — | — | 1 | 5.22 |
| CHEMBL1801431 | — | — | 1 | 5.22 |
| CHEMBL1229868 | — | — | 1 | 5.10 |
| CHEMBL1082381 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1801044 | — | IC50 | = | 268.0 | nM | 6.57 |
| CHEMBL1801049 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL1801048 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1801046 | — | IC50 | = | 435.0 | nM | 6.36 |
| CHEMBL1801417 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL1801422 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1801412 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL1801052 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL1801050 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL1801045 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL1801416 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1801420 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL1801421 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL1801053 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1801397 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL1801047 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1801396 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1801056 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL1801430 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1801419 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL1801395 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL1801057 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL1801393 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL1801054 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1801055 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1801394 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL1801423 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1801431 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1229868 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL1082381 | — | IC50 | = | 8660.0 | nM | 5.06 |
| CHEMBL1801414 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1801429 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1801424 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801418 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801425 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1800089 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801415 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801413 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801426 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801427 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801428 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801051 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1771212 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801398 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1801399 | — | IC50 | > | 10000.0 | nM | - |