Assay Detail
Binding
CHEMBL4307491
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human TRPV4 expressed in baculovirus infected HEK/MSR 2 cells pre-incubated for 10 mins followed by GSK634775A addition by Fura-2 dye based FLIPR assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Transient receptor potential cation channel subfamily V member 4 (CHEMBL3119) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.59 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4469630 | — | — | 1 | 9.30 |
| CHEMBL4588831 | — | — | 1 | 8.92 |
| CHEMBL4521512 | — | — | 1 | 8.92 |
| CHEMBL4536058 | — | — | 1 | 8.82 |
| CHEMBL4532369 | — | — | 1 | 8.80 |
| CHEMBL4541827 | — | — | 1 | 8.77 |
| CHEMBL4470585 | GSK2798745 | 2.0 | 1 | 8.74 |
| CHEMBL4514491 | — | — | 1 | 8.60 |
| CHEMBL4588158 | — | — | 1 | 8.51 |
| CHEMBL4469982 | — | — | 1 | 8.38 |
| CHEMBL4560266 | — | — | 1 | 8.28 |
| CHEMBL4579838 | — | — | 1 | 8.28 |
| CHEMBL4447221 | — | — | 1 | 7.85 |
| CHEMBL4549613 | — | — | 1 | 7.80 |
| CHEMBL4465488 | — | — | 1 | 7.32 |
| CHEMBL4544597 | — | — | 1 | 7.31 |
| CHEMBL4519711 | — | — | 1 | 7.22 |
| CHEMBL4447940 | — | — | 1 | 7.22 |
| CHEMBL4535351 | — | — | 1 | 7.20 |
| CHEMBL4556983 | — | — | 1 | 7.13 |
| CHEMBL4590243 | — | — | 1 | 7.02 |
| CHEMBL4471311 | — | — | 1 | 6.85 |
| CHEMBL4581258 | — | — | 1 | 6.62 |
| CHEMBL4571300 | — | — | 1 | 6.51 |
| CHEMBL4450392 | — | — | 1 | 6.47 |
| CHEMBL4520028 | — | — | 1 | 6.27 |
| CHEMBL4549957 | — | — | 1 | 6.09 |
| CHEMBL4462803 | — | — | 1 | 5.72 |
| CHEMBL4522756 | — | — | 1 | 5.28 |
| CHEMBL4471400 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4469630 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4588831 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4521512 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4536058 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4532369 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4541827 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4470585 | GSK2798745 | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4514491 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4588158 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4469982 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4560266 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4579838 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4447221 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4549613 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4465488 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4544597 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4519711 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4447940 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4535351 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4556983 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4590243 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4471311 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4581258 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4571300 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4450392 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4520028 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4549957 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL4462803 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4522756 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4471400 | — | IC50 | > | 25000.0 | nM | - |