Assay Detail
Functional
CHEMBL912134
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against low pH(5.0-5.5)-activated rat VR1
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL5102) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 64 | 7.12 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214989 | — | — | 1 | 9.40 |
| CHEMBL214331 | — | — | 1 | 9.00 |
| CHEMBL214796 | NGD-8243 | 2.0 | 1 | 8.85 |
| CHEMBL183752 | — | — | 1 | 8.70 |
| CHEMBL386251 | — | — | 1 | 8.40 |
| CHEMBL180902 | — | — | 1 | 8.40 |
| CHEMBL183045 | — | — | 1 | 8.30 |
| CHEMBL214628 | — | — | 1 | 8.30 |
| CHEMBL183121 | — | — | 1 | 8.10 |
| CHEMBL180138 | — | — | 1 | 8.05 |
| CHEMBL427052 | — | — | 1 | 8.05 |
| CHEMBL214607 | — | — | 1 | 7.96 |
| CHEMBL386040 | — | — | 1 | 7.89 |
| CHEMBL214274 | — | — | 1 | 7.70 |
| CHEMBL378563 | — | — | 1 | 7.58 |
| CHEMBL214658 | — | — | 1 | 7.47 |
| CHEMBL214510 | — | — | 1 | 7.46 |
| CHEMBL215330 | — | — | 1 | 7.44 |
| CHEMBL217201 | — | — | 1 | 7.43 |
| CHEMBL213975 | — | — | 1 | 7.37 |
| CHEMBL213718 | — | — | 1 | 7.36 |
| CHEMBL215482 | — | — | 1 | 7.25 |
| CHEMBL212072 | — | — | 1 | 7.23 |
| CHEMBL215777 | — | — | 1 | 7.22 |
| CHEMBL386017 | — | — | 1 | 7.19 |
| CHEMBL215063 | — | — | 1 | 7.09 |
| CHEMBL385717 | — | — | 1 | 7.06 |
| CHEMBL216882 | — | — | 1 | 6.99 |
| CHEMBL214563 | — | — | 1 | 6.85 |
| CHEMBL267538 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214989 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL214331 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL214796 | NGD-8243 | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL183752 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL386251 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL180902 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL183045 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL214628 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL183121 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL180138 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL427052 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL214607 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL386040 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL214274 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL378563 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL214658 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL214510 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL215330 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL217201 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL213975 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL213718 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL215482 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL212072 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL215777 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL386017 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL215063 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL385717 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL216882 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL214563 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL267538 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL214880 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL214852 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL215422 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL384600 | — | IC50 | = | 196.0 | nM | 6.71 |
| CHEMBL384700 | — | IC50 | = | 222.0 | nM | 6.65 |
| CHEMBL212564 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL215650 | — | IC50 | = | 263.0 | nM | 6.58 |
| CHEMBL386795 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL425258 | — | IC50 | = | 325.0 | nM | 6.49 |
| CHEMBL212910 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL215966 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL387433 | — | IC50 | = | 366.0 | nM | 6.44 |
| CHEMBL215433 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL385241 | — | IC50 | = | 583.0 | nM | 6.23 |
| CHEMBL384319 | — | IC50 | = | 639.0 | nM | 6.19 |
| CHEMBL276153 | — | IC50 | = | 694.0 | nM | 6.16 |
| CHEMBL215047 | — | IC50 | = | 722.0 | nM | 6.14 |
| CHEMBL384966 | — | IC50 | = | 764.0 | nM | 6.12 |
| CHEMBL215439 | — | IC50 | = | 896.0 | nM | 6.05 |
| CHEMBL215751 | — | IC50 | = | 1044.0 | nM | 5.98 |