Assay Detail
Binding
CHEMBL3265736
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of DDR2 T654M mutant (unknown origin) preincubated for 30 mins before substrate addition by FRET assay
28
Total Activities
28
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 |
Target
Discoidin domain-containing receptor 2 (CHEMBL5122) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of type II and III DDR2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.69 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2403816 | — | — | 1 | 9.00 |
| CHEMBL1738943 | — | — | 1 | 8.70 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 7.89 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.75 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.75 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.44 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.29 |
| CHEMBL2403875 | — | — | 1 | 7.14 |
| CHEMBL344800 | — | — | 1 | 7.14 |
| CHEMBL3261116 | — | — | 1 | 7.12 |
| CHEMBL1940500 | — | — | 1 | 6.64 |
| CHEMBL1940504 | — | — | 1 | 6.42 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.35 |
| CHEMBL1738945 | — | — | 1 | 6.17 |
| CHEMBL3261118 | — | — | 1 | 6.16 |
| CHEMBL498947 | — | — | 1 | 6.14 |
| CHEMBL1738942 | — | — | 1 | 6.09 |
| CHEMBL568875 | — | — | 1 | 6.09 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.08 |
| CHEMBL1738946 | — | — | 1 | 5.94 |
| CHEMBL583263 | — | — | 1 | 5.91 |
| CHEMBL1940503 | — | — | 1 | 5.78 |
| CHEMBL1940505 | — | — | 1 | 5.74 |
| CHEMBL87580 | — | — | 1 | 5.60 |
| CHEMBL522387 | — | — | 1 | 4.97 |
| CHEMBL476011 | — | — | 1 | - |
| CHEMBL420047 | — | — | 1 | - |
| CHEMBL578172 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2403816 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1738943 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL103667 | DORAMAPIMOD | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL255863 | NILOTINIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL572878 | TOZASERTIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL477772 | PAZOPANIB | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2403875 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL344800 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL3261116 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1940500 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1940504 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL253969 | OSI-632 | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1738945 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL3261118 | — | IC50 | = | 687.0 | nM | 6.16 |
| CHEMBL498947 | — | IC50 | = | 717.0 | nM | 6.14 |
| CHEMBL1738942 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL568875 | — | IC50 | = | 808.0 | nM | 6.09 |
| CHEMBL5416410 | DASATINIB | IC50 | = | 833.0 | nM | 6.08 |
| CHEMBL1738946 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL583263 | — | IC50 | = | 1233.0 | nM | 5.91 |
| CHEMBL1940503 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL1940505 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL87580 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL522387 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL476011 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL420047 | — | IC50 | >= | 100000.0 | nM | - |
| CHEMBL578172 | — | IC50 | >= | 100000.0 | nM | - |