Assay Detail
Functional
CHEMBL4371834
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and optimization of pyrazole amides as antagonists of CCR1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 7.01 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4571977 | — | — | 1 | 9.10 |
| CHEMBL232656 | BX 471 FREE BASE | 2.0 | 1 | 8.89 |
| CHEMBL4444976 | CCX354 | 2.0 | 1 | 8.70 |
| CHEMBL3334824 | BMS-817399 | 2.0 | 1 | 8.52 |
| CHEMBL4436061 | — | — | 1 | 8.00 |
| CHEMBL4577357 | — | — | 1 | 7.89 |
| CHEMBL4568048 | — | — | 1 | 7.82 |
| CHEMBL4513370 | — | — | 1 | 7.55 |
| CHEMBL4583870 | — | — | 1 | 7.33 |
| CHEMBL1628706 | — | — | 1 | 7.23 |
| CHEMBL4456839 | — | — | 1 | 6.46 |
| CHEMBL4574870 | — | — | 1 | 6.38 |
| CHEMBL4539264 | — | — | 1 | 6.30 |
| CHEMBL4440166 | — | — | 1 | 6.22 |
| CHEMBL4449368 | — | — | 1 | 6.10 |
| CHEMBL4538794 | — | — | 1 | 6.02 |
| CHEMBL4464403 | — | — | 1 | 5.92 |
| CHEMBL4565390 | — | — | 1 | 5.77 |
| CHEMBL4468514 | — | — | 1 | 5.72 |
| CHEMBL4571547 | — | — | 1 | 5.68 |
| CHEMBL4462565 | — | — | 1 | 5.62 |
| CHEMBL4515118 | — | — | 1 | - |
| CHEMBL4452387 | — | — | 1 | - |
| CHEMBL4589222 | — | — | 1 | - |
| CHEMBL4476819 | — | — | 1 | - |
| CHEMBL4453448 | — | — | 1 | - |
| CHEMBL4457735 | — | — | 1 | - |
| CHEMBL4469919 | — | — | 1 | - |
| CHEMBL4436168 | — | — | 1 | - |
| CHEMBL4440305 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4571977 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL232656 | BX 471 FREE BASE | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4444976 | CCX354 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3334824 | BMS-817399 | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4436061 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4577357 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4568048 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4513370 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4583870 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL1628706 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4456839 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4574870 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4539264 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4440166 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL4449368 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL4538794 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4464403 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4565390 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4468514 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4571547 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4462565 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4579581 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4461535 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4468178 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4540639 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4525819 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4462862 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4591612 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4441611 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4441466 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4556112 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4548382 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4441483 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4586777 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4592988 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4587236 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4577782 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4440305 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4436168 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4469919 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4457735 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4453448 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4476819 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4589222 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4452387 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4515118 | — | IC50 | > | 3000.0 | nM | - |