Assay Detail
Functional
CHEMBL976411
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Antagonist activity at human TRPV1 receptor assessed as inhibition of capsaicin-induced activation
42
Total Activities
42
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 |
Target
Transient receptor potential cation channel subfamily V member 1 (CHEMBL4794) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 8.10 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL457188 | — | — | 1 | 9.52 |
| CHEMBL456162 | — | — | 1 | 9.40 |
| CHEMBL526827 | — | — | 1 | 9.30 |
| CHEMBL456778 | — | — | 1 | 9.30 |
| CHEMBL214796 | NGD-8243 | 2.0 | 1 | 9.10 |
| CHEMBL498666 | — | — | 1 | 9.05 |
| CHEMBL457003 | — | — | 1 | 9.00 |
| CHEMBL513942 | — | — | 1 | 9.00 |
| CHEMBL457842 | — | — | 1 | 8.92 |
| CHEMBL497650 | — | — | 1 | 8.82 |
| CHEMBL456152 | — | — | 1 | 8.70 |
| CHEMBL446258 | — | — | 1 | 8.70 |
| CHEMBL456128 | — | — | 1 | 8.70 |
| CHEMBL458058 | — | — | 1 | 8.68 |
| CHEMBL456571 | — | — | 1 | 8.60 |
| CHEMBL456570 | — | — | 1 | 8.52 |
| CHEMBL497649 | — | — | 1 | 8.40 |
| CHEMBL456961 | — | — | 1 | 8.35 |
| CHEMBL456764 | — | — | 1 | 8.22 |
| CHEMBL463382 | — | — | 1 | 8.15 |
| CHEMBL451895 | — | — | 1 | 8.10 |
| CHEMBL456546 | — | — | 1 | 8.10 |
| CHEMBL457002 | — | — | 1 | 8.05 |
| CHEMBL456572 | — | — | 1 | 7.92 |
| CHEMBL378563 | — | — | 1 | 7.85 |
| CHEMBL456358 | — | — | 1 | 7.66 |
| CHEMBL456127 | — | — | 1 | 7.62 |
| CHEMBL464386 | — | — | 1 | 7.60 |
| CHEMBL463578 | — | — | 1 | 7.60 |
| CHEMBL457843 | — | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL457188 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL456162 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL456778 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL526827 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL214796 | NGD-8243 | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL498666 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL457003 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL513942 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL457842 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL497650 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL446258 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL456128 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL456152 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL458058 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL456571 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL456570 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL497649 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL456961 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL456764 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL463382 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL456546 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL451895 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL457002 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL456572 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL378563 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL456358 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL456127 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL464386 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL463578 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL457843 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL462981 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL456545 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL462783 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL456982 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL457197 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL456990 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL514248 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL456151 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL458925 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL456962 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL464592 | — | IC50 | = | 1627.0 | nM | 5.79 |
| CHEMBL515050 | — | IC50 | > | 3000.0 | nM | - |