Assay Detail
Functional
CHEMBL5378340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GPR183 expressed in CHO-K1 cells co-expressing Gqi5 assessed as inhibition of 7alpha,25-OHC induced calcium mobilization incubated for 30 mins by FLIPR Calcium 6 dye based assay
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a First-in-Class GPR183 Antagonist for the Potential Treatment of Rheumatoid Arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 6.99 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5401247 | — | — | 1 | 7.80 |
| CHEMBL5421607 | — | — | 1 | 7.68 |
| CHEMBL5424378 | — | — | 1 | 7.66 |
| CHEMBL5406913 | — | — | 1 | 7.59 |
| CHEMBL5399120 | — | — | 1 | 7.53 |
| CHEMBL5395781 | — | — | 1 | 7.52 |
| CHEMBL5394700 | — | — | 1 | 7.50 |
| CHEMBL5405057 | — | — | 1 | 7.48 |
| CHEMBL5414588 | — | — | 1 | 7.41 |
| CHEMBL3262896 | — | — | 1 | 7.41 |
| CHEMBL5439756 | — | — | 1 | 7.35 |
| CHEMBL5397313 | — | — | 1 | 7.28 |
| CHEMBL5402356 | — | — | 1 | 7.26 |
| CHEMBL5412445 | — | — | 1 | 7.24 |
| CHEMBL5438584 | — | — | 1 | 7.22 |
| CHEMBL5400278 | — | — | 1 | 7.19 |
| CHEMBL5395361 | — | — | 1 | 7.18 |
| CHEMBL5400459 | — | — | 1 | 7.16 |
| CHEMBL5395357 | — | — | 1 | 7.15 |
| CHEMBL5405959 | — | — | 1 | 7.09 |
| CHEMBL5431534 | — | — | 1 | 6.99 |
| CHEMBL5435007 | — | — | 1 | 6.98 |
| CHEMBL5430675 | — | — | 1 | 6.96 |
| CHEMBL5425366 | — | — | 1 | 6.91 |
| CHEMBL5425720 | — | — | 1 | 6.89 |
| CHEMBL5413510 | — | — | 1 | 6.88 |
| CHEMBL5422521 | — | — | 1 | 6.87 |
| CHEMBL5395113 | — | — | 1 | 6.80 |
| CHEMBL5412345 | — | — | 1 | 6.70 |
| CHEMBL5423746 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5401247 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5421607 | — | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL5424378 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5406913 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL5399120 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL5395781 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5394700 | — | IC50 | = | 31.3 | nM | 7.50 |
| CHEMBL5405057 | — | IC50 | = | 33.3 | nM | 7.48 |
| CHEMBL5414588 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3262896 | — | IC50 | = | 38.6 | nM | 7.41 |
| CHEMBL5439756 | — | IC50 | = | 45.1 | nM | 7.35 |
| CHEMBL5397313 | — | IC50 | = | 52.4 | nM | 7.28 |
| CHEMBL5402356 | — | IC50 | = | 54.6 | nM | 7.26 |
| CHEMBL5412445 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5438584 | — | IC50 | = | 60.5 | nM | 7.22 |
| CHEMBL5400278 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5395361 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5400459 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5395357 | — | IC50 | = | 70.1 | nM | 7.15 |
| CHEMBL5405959 | — | IC50 | = | 81.8 | nM | 7.09 |
| CHEMBL5431534 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL5435007 | — | IC50 | = | 105.0 | nM | 6.98 |
| CHEMBL5430675 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5425366 | — | IC50 | = | 122.8 | nM | 6.91 |
| CHEMBL5425720 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL5413510 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL5422521 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL5395113 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL5412345 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5423746 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL5394888 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL5402708 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL5423491 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL5416074 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5415152 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL5400812 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL5432988 | — | IC50 | = | 439.0 | nM | 6.36 |
| CHEMBL5419703 | — | IC50 | = | 467.0 | nM | 6.33 |
| CHEMBL5434815 | — | IC50 | = | 498.0 | nM | 6.30 |
| CHEMBL5426423 | — | IC50 | = | 562.0 | nM | 6.25 |
| CHEMBL5413214 | — | IC50 | = | 739.0 | nM | 6.13 |
| CHEMBL5411108 | — | IC50 | = | 865.0 | nM | 6.06 |
| CHEMBL5411275 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5415456 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5429633 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5427473 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5419916 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5425163 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5402863 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5413267 | — | IC50 | > | 1000.0 | nM | - |