Assay Detail
Binding
CHEMBL2444634
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of APMA-activated recombinant human MMP2 using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2 as substrate incubated for 30 mins prior to substrate addition measured after 2 to 4 hrs by fluorometric assay
24
Total Activities
24
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
Arylamino methylene bisphosphonate derivatives as bone seeking matrix metalloproteinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 4.95 | 5.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2440431 | — | — | 1 | 5.68 |
| CHEMBL2440432 | — | — | 1 | 5.55 |
| CHEMBL2440430 | — | — | 1 | 5.55 |
| CHEMBL2440441 | — | — | 1 | 5.22 |
| CHEMBL2440429 | — | — | 1 | 5.19 |
| CHEMBL2440438 | — | — | 1 | 5.18 |
| CHEMBL4303669 | ZOLEDRONIC ACID | 4.0 | 1 | 5.16 |
| CHEMBL1350 | TILUDRONIC ACID | 4.0 | 1 | 5.14 |
| CHEMBL2440440 | — | — | 1 | 4.82 |
| CHEMBL450938 | (3-NITROPHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | — | 1 | 4.81 |
| CHEMBL2440578 | — | — | 1 | 4.70 |
| CHEMBL2440435 | — | — | 1 | 4.68 |
| CHEMBL2440434 | — | — | 1 | 4.60 |
| CHEMBL2440581 | — | — | 1 | 4.55 |
| CHEMBL2440437 | — | — | 1 | 4.44 |
| CHEMBL370662 | — | — | 1 | 4.43 |
| CHEMBL2440436 | — | — | 1 | 4.38 |
| CHEMBL2440433 | 3,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | — | 1 | - |
| CHEMBL2440439 | (P-TOLYLAMINO)METHYLENEDIPHOSPHONIC ACID | — | 1 | - |
| CHEMBL191613 | 2,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | — | 1 | - |
| CHEMBL2440579 | (4-CHLOROPHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | — | 1 | - |
| CHEMBL2440580 | (PHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | — | 1 | - |
| CHEMBL293479 | — | — | 1 | - |
| CHEMBL55371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2440431 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL2440432 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2440430 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL2440441 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL2440429 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL2440438 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4303669 | ZOLEDRONIC ACID | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL1350 | TILUDRONIC ACID | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL2440440 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL450938 | (3-NITROPHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL2440578 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL2440435 | — | IC50 | = | 20800.0 | nM | 4.68 |
| CHEMBL2440434 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2440581 | — | IC50 | = | 28200.0 | nM | 4.55 |
| CHEMBL2440437 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL370662 | — | IC50 | = | 37400.0 | nM | 4.43 |
| CHEMBL2440436 | — | IC50 | = | 42000.0 | nM | 4.38 |
| CHEMBL2440433 | 3,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | IC50 | > | 100000.0 | nM | - |
| CHEMBL2440439 | (P-TOLYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | > | 100000.0 | nM | - |
| CHEMBL191613 | 2,4-DICHLOROPHENYLAMINOMETHYLENEBISPHOSPHONIC ACID | IC50 | > | 100000.0 | nM | - |
| CHEMBL2440579 | (4-CHLOROPHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | > | 100000.0 | nM | - |
| CHEMBL2440580 | (PHENYLAMINO)METHYLENEDIPHOSPHONIC ACID | IC50 | > | 100000.0 | nM | - |
| CHEMBL293479 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL55371 | — | IC50 | > | 100000.0 | nM | - |