Assay Detail
Functional
CHEMBL912133
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against capsaicin-activated human VR1 by FLIPR assay
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 64 | 6.95 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214989 | — | — | 1 | 9.10 |
| CHEMBL214796 | NGD-8243 | 2.0 | 1 | 8.96 |
| CHEMBL214331 | — | — | 1 | 8.52 |
| CHEMBL183045 | — | — | 1 | 8.30 |
| CHEMBL180902 | — | — | 1 | 8.22 |
| CHEMBL183752 | — | — | 1 | 8.10 |
| CHEMBL183121 | — | — | 1 | 7.96 |
| CHEMBL180138 | — | — | 1 | 7.96 |
| CHEMBL378563 | — | — | 1 | 7.85 |
| CHEMBL214607 | — | — | 1 | 7.77 |
| CHEMBL386017 | — | — | 1 | 7.62 |
| CHEMBL386040 | — | — | 1 | 7.52 |
| CHEMBL427052 | — | — | 1 | 7.41 |
| CHEMBL215777 | — | — | 1 | 7.38 |
| CHEMBL215330 | — | — | 1 | 7.37 |
| CHEMBL386251 | — | — | 1 | 7.31 |
| CHEMBL214628 | — | — | 1 | 7.31 |
| CHEMBL217147 | — | — | 1 | 7.24 |
| CHEMBL215482 | — | — | 1 | 7.22 |
| CHEMBL214274 | — | — | 1 | 7.21 |
| CHEMBL215063 | — | — | 1 | 7.19 |
| CHEMBL213975 | — | — | 1 | 7.14 |
| CHEMBL214880 | — | — | 1 | 7.04 |
| CHEMBL212072 | — | — | 1 | 7.04 |
| CHEMBL216882 | — | — | 1 | 7.03 |
| CHEMBL425258 | — | — | 1 | 6.91 |
| CHEMBL215966 | — | — | 1 | 6.88 |
| CHEMBL214510 | — | — | 1 | 6.82 |
| CHEMBL217201 | — | — | 1 | 6.80 |
| CHEMBL214563 | — | — | 1 | 6.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214989 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL214796 | NGD-8243 | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL214331 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL183045 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL180902 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL183752 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL183121 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL180138 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL378563 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL214607 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL386017 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL386040 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL427052 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL215777 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL215330 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL386251 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL214628 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL217147 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL215482 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL214274 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL215063 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL213975 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL214880 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL212072 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL216882 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL425258 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL215966 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL214510 | — | IC50 | = | 152.0 | nM | 6.82 |
| CHEMBL217201 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL214563 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL385717 | — | IC50 | = | 168.0 | nM | 6.78 |
| CHEMBL387433 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL213718 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL214852 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL215650 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL215422 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL267538 | — | IC50 | = | 377.0 | nM | 6.42 |
| CHEMBL214658 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL384700 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL385966 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL385241 | — | IC50 | = | 624.0 | nM | 6.21 |
| CHEMBL212564 | — | IC50 | = | 746.0 | nM | 6.13 |
| CHEMBL215439 | — | IC50 | = | 974.0 | nM | 6.01 |
| CHEMBL215047 | — | IC50 | = | 1015.0 | nM | 5.99 |
| CHEMBL386795 | — | IC50 | = | 1106.0 | nM | 5.96 |
| CHEMBL212910 | — | IC50 | = | 1412.0 | nM | 5.85 |
| CHEMBL384600 | — | IC50 | = | 1527.0 | nM | 5.82 |
| CHEMBL214686 | — | IC50 | = | 1502.0 | nM | 5.82 |
| CHEMBL213660 | — | IC50 | = | 1779.0 | nM | 5.75 |
| CHEMBL215015 | — | IC50 | = | 2585.0 | nM | 5.59 |