Assay Detail
Binding
CHEMBL3383300
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of menthol induced Ca2+ influx
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily M member 8 (CHEMBL1075319) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 6.88 | 9.02 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353600 | — | — | 1 | 9.02 |
| CHEMBL3353601 | — | — | 1 | 8.48 |
| CHEMBL3353610 | — | — | 1 | 8.21 |
| CHEMBL3353602 | — | — | 1 | 8.10 |
| CHEMBL3353597 | — | — | 1 | 8.08 |
| CHEMBL3353594 | — | — | 1 | 8.05 |
| CHEMBL3353609 | — | — | 1 | 7.96 |
| CHEMBL3353599 | — | — | 1 | 7.85 |
| CHEMBL3353606 | — | — | 1 | 7.82 |
| CHEMBL3353608 | — | — | 1 | 7.80 |
| CHEMBL3353607 | — | — | 1 | 7.75 |
| CHEMBL3353592 | — | — | 1 | 7.57 |
| CHEMBL3353598 | — | — | 1 | 7.40 |
| CHEMBL3353593 | — | — | 1 | 7.39 |
| CHEMBL3353573 | — | — | 1 | 7.38 |
| CHEMBL3353605 | — | — | 1 | 7.34 |
| CHEMBL3353589 | — | — | 1 | 7.31 |
| CHEMBL3353596 | — | — | 1 | 7.24 |
| CHEMBL3353575 | — | — | 1 | 7.24 |
| CHEMBL3353572 | — | — | 1 | 7.21 |
| CHEMBL3353603 | — | — | 1 | 7.17 |
| CHEMBL3353576 | — | — | 1 | 7.17 |
| CHEMBL3353574 | — | — | 1 | 7.16 |
| CHEMBL3353595 | — | — | 1 | 7.02 |
| CHEMBL3353590 | — | — | 1 | 6.98 |
| CHEMBL3353582 | — | — | 1 | 6.91 |
| CHEMBL3353569 | — | — | 1 | 6.74 |
| CHEMBL3353579 | — | — | 1 | 6.70 |
| CHEMBL3353577 | — | — | 1 | 6.67 |
| CHEMBL3353583 | — | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353600 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL3353601 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3353610 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL3353602 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3353597 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL3353594 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3353609 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3353599 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3353606 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3353608 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3353607 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3353592 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3353598 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3353593 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3353573 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3353605 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3353589 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL3353596 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3353575 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3353572 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3353576 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3353603 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3353574 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3353595 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL3353590 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL3353582 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3353569 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL3353579 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL3353577 | — | IC50 | = | 216.0 | nM | 6.67 |
| CHEMBL3353583 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL3353571 | — | IC50 | = | 406.0 | nM | 6.39 |
| CHEMBL3353581 | — | IC50 | = | 707.0 | nM | 6.15 |
| CHEMBL3353584 | — | IC50 | = | 736.0 | nM | 6.13 |
| CHEMBL3353588 | — | IC50 | = | 762.0 | nM | 6.12 |
| CHEMBL3353587 | — | IC50 | = | 1562.0 | nM | 5.81 |
| CHEMBL3353585 | — | IC50 | = | 2472.0 | nM | 5.61 |
| CHEMBL3353586 | — | IC50 | = | 2983.0 | nM | 5.53 |
| CHEMBL3353591 | — | IC50 | = | 3720.0 | nM | 5.43 |
| CHEMBL3352829 | — | IC50 | = | 8419.0 | nM | 5.08 |
| CHEMBL3353578 | — | IC50 | = | 9859.0 | nM | 5.01 |
| CHEMBL3353570 | — | IC50 | = | 15974.0 | nM | 4.80 |
| CHEMBL3353604 | — | IC50 | = | 18216.0 | nM | 4.74 |
| CHEMBL3353580 | — | IC50 | = | 23782.0 | nM | 4.62 |