Assay Detail
Binding
CHEMBL869873
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Displacement of [125I]SP from human cloned NK1 receptor expressed in CHO cells
42
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Cyclopentane-based human NK1 antagonists. Part 1: discovery and initial SAR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 8.37 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52330 | — | — | 1 | 10.05 |
| CHEMBL1471 | APREPITANT | 4.0 | 1 | 10.05 |
| CHEMBL213726 | — | — | 1 | 9.11 |
| CHEMBL212931 | — | — | 1 | 9.09 |
| CHEMBL426145 | — | — | 1 | 9.08 |
| CHEMBL213134 | — | — | 1 | 9.05 |
| CHEMBL212839 | — | — | 2 | 9.02 |
| CHEMBL211304 | — | — | 1 | 8.96 |
| CHEMBL377881 | — | — | 1 | 8.82 |
| CHEMBL209531 | — | — | 1 | 8.72 |
| CHEMBL212439 | — | — | 1 | 8.72 |
| CHEMBL212919 | — | — | 1 | 8.72 |
| CHEMBL209627 | — | — | 1 | 8.70 |
| CHEMBL379707 | — | — | 1 | 8.68 |
| CHEMBL438789 | — | — | 2 | 8.64 |
| CHEMBL384102 | — | — | 1 | 8.62 |
| CHEMBL384157 | — | — | 1 | 8.57 |
| CHEMBL212644 | — | — | 1 | 8.57 |
| CHEMBL213316 | — | — | 1 | 8.57 |
| CHEMBL424709 | — | — | 1 | 8.46 |
| CHEMBL378340 | — | — | 1 | 8.33 |
| CHEMBL377916 | — | — | 1 | 8.31 |
| CHEMBL378537 | — | — | 1 | 8.30 |
| CHEMBL214317 | — | — | 1 | 8.30 |
| CHEMBL215315 | — | — | 1 | 8.28 |
| CHEMBL211257 | — | — | 1 | 8.28 |
| CHEMBL378076 | — | — | 1 | 8.21 |
| CHEMBL429715 | — | — | 1 | 8.14 |
| CHEMBL213359 | — | — | 1 | 8.14 |
| CHEMBL384796 | — | — | 1 | 8.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52330 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL1471 | APREPITANT | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL213726 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL212931 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL426145 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL213134 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL212839 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL211304 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL212839 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL377881 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL212919 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL212439 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL209531 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL209627 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL379707 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL438789 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL384102 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL384157 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL212644 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL213316 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL424709 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL378340 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL377916 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL378537 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL214317 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL215315 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL211257 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL438789 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL378076 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL429715 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL213359 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL384796 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL212978 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL213908 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL380017 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL386258 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL384244 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL379744 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL378984 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL424883 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL214435 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL212697 | — | IC50 | = | 300.0 | nM | 6.52 |