Assay Detail
Binding
CHEMBL4617064
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human MMP2 catalytic domain (Tyr110 to Asp452 residues) expressed in yeast cells using Mca-Pro-Leu-Gly-Leu-Dpa-Ala-Arg-NH2/TQ3-GABA-Pro-Cha-Abu-Smc-His-Ala-Dab(6'-TAMRA)-Ala-Lys-NH2 as fluorogenic substrate preincubated for 15 mins followed by substrate addition measured after 2 to 4 hrs by fluorometric analysis
44
Total Activities
44
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
Virtual screening identification and chemical optimization of substituted 2-arylbenzimidazoles as new non-zinc-binding MMP-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 4.78 | 5.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4634914 | — | — | 1 | 5.51 |
| CHEMBL4647123 | — | — | 1 | 5.48 |
| CHEMBL4639311 | — | — | 1 | 5.41 |
| CHEMBL1483847 | — | — | 1 | 5.38 |
| CHEMBL1965818 | — | — | 1 | 5.24 |
| CHEMBL477841 | — | — | 1 | 5.19 |
| CHEMBL4642399 | — | — | 1 | 5.19 |
| CHEMBL4640667 | — | — | 1 | 5.19 |
| CHEMBL4285334 | — | — | 1 | 5.19 |
| CHEMBL4637824 | — | — | 1 | 5.16 |
| CHEMBL4636483 | — | — | 1 | 5.07 |
| CHEMBL4635076 | — | — | 1 | 5.06 |
| CHEMBL4635438 | — | — | 1 | 5.05 |
| CHEMBL4648156 | — | — | 1 | 5.05 |
| CHEMBL4643922 | — | — | 1 | 5.03 |
| CHEMBL522613 | — | — | 1 | 5.01 |
| CHEMBL4646265 | — | — | 1 | 5.00 |
| CHEMBL204153 | — | — | 1 | 4.92 |
| CHEMBL4645291 | — | — | 1 | 4.85 |
| CHEMBL4640215 | — | — | 1 | 4.80 |
| CHEMBL4633399 | — | — | 1 | 4.80 |
| CHEMBL421666 | — | — | 1 | 4.79 |
| CHEMBL4647266 | — | — | 1 | 4.72 |
| CHEMBL4640970 | — | — | 1 | 4.60 |
| CHEMBL4646530 | — | — | 1 | 4.51 |
| CHEMBL4632565 | — | — | 1 | 4.51 |
| CHEMBL4639945 | — | — | 1 | 4.51 |
| CHEMBL4647857 | — | — | 1 | 4.50 |
| CHEMBL4636104 | — | — | 1 | 4.35 |
| CHEMBL4640244 | — | — | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4634914 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4647123 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4639311 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1483847 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1965818 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL477841 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4642399 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4640667 | — | IC50 | = | 6420.0 | nM | 5.19 |
| CHEMBL4285334 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4637824 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4636483 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4635076 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL4635438 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL4648156 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL4643922 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL522613 | — | IC50 | = | 9700.0 | nM | 5.01 |
| CHEMBL4646265 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL204153 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL4645291 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4640215 | — | IC50 | = | 15900.0 | nM | 4.80 |
| CHEMBL4633399 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL421666 | — | IC50 | = | 16400.0 | nM | 4.79 |
| CHEMBL4647266 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4640970 | — | IC50 | = | 25300.0 | nM | 4.60 |
| CHEMBL4646530 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4632565 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4639945 | — | IC50 | = | 31000.0 | nM | 4.51 |
| CHEMBL4647857 | — | IC50 | = | 31500.0 | nM | 4.50 |
| CHEMBL4636104 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL4640244 | — | IC50 | = | 47000.0 | nM | 4.33 |
| CHEMBL4638078 | — | IC50 | = | 48000.0 | nM | 4.32 |
| CHEMBL4644146 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL4638748 | — | IC50 | = | 64000.0 | nM | 4.19 |
| CHEMBL1277658 | — | IC50 | = | 65400.0 | nM | 4.18 |
| CHEMBL4641067 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL473361 | — | IC50 | = | 82000.0 | nM | 4.09 |
| CHEMBL4632444 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL4634529 | — | IC50 | = | 96000.0 | nM | 4.02 |
| CHEMBL4636536 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4641864 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL93118 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4638723 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4646018 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4648990 | — | IC50 | > | 100000.0 | nM | - |