Assay Detail
Functional
CHEMBL4332212
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
50
Total Activities
50
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
Identification of novel azaindazole CCR1 antagonist clinical candidates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 50 | 7.55 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4464625 | — | — | 1 | 9.70 |
| CHEMBL4457209 | — | — | 1 | 9.70 |
| CHEMBL4475581 | — | — | 1 | 9.52 |
| CHEMBL4518015 | — | — | 1 | 8.92 |
| CHEMBL4562738 | — | — | 1 | 8.85 |
| CHEMBL4456123 | BI 639667 | 1.0 | 1 | 8.74 |
| CHEMBL4475173 | — | — | 1 | 8.70 |
| CHEMBL4474606 | — | — | 1 | 8.70 |
| CHEMBL4448761 | — | — | 1 | 8.52 |
| CHEMBL4475237 | — | — | 1 | 8.35 |
| CHEMBL4465000 | — | — | 1 | 8.30 |
| CHEMBL4475918 | — | — | 1 | 8.22 |
| CHEMBL4441094 | — | — | 1 | 8.17 |
| CHEMBL4475801 | — | — | 1 | 8.10 |
| CHEMBL4464575 | — | — | 1 | 7.92 |
| CHEMBL4586189 | — | — | 1 | 7.92 |
| CHEMBL4442765 | — | — | 1 | 7.92 |
| CHEMBL4449996 | — | — | 1 | 7.77 |
| CHEMBL4466500 | — | — | 1 | 7.72 |
| CHEMBL4448064 | — | — | 1 | 7.66 |
| CHEMBL4454067 | — | — | 1 | 7.47 |
| CHEMBL4472994 | — | — | 1 | 7.39 |
| CHEMBL4565496 | — | — | 1 | 7.36 |
| CHEMBL4437170 | — | — | 1 | 7.26 |
| CHEMBL4559388 | — | — | 1 | 7.21 |
| CHEMBL4519965 | — | — | 1 | 7.21 |
| CHEMBL4469176 | — | — | 1 | 7.17 |
| CHEMBL4471579 | — | — | 1 | 6.92 |
| CHEMBL4544186 | — | — | 1 | 6.77 |
| CHEMBL4577460 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4464625 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4457209 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4475581 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4518015 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4562738 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4456123 | BI 639667 | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4475173 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4474606 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4448761 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4475237 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4465000 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4475918 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4441094 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4475801 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4442765 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4464575 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4586189 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4449996 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4466500 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4448064 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4454067 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4472994 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4565496 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4437170 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL4519965 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4559388 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4469176 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4471579 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4544186 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4577460 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4591935 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4557554 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4445316 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4568987 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4458721 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4552741 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4450029 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4527255 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4440452 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4445779 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4457889 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4476649 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4475146 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4533629 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4463439 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4518812 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4440565 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4533401 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4514702 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL4563543 | — | IC50 | > | 3000.0 | nM | - |