Assay Detail
Binding
CHEMBL5149726
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibitor ethyl isopropyl amiloride by BCECF-AM dye based fluorescence assay
46
Total Activities
46
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Kidney |
| Cell Type | Kidney epithelial cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Tenapanor: A First-in-Class Minimally Systemic Inhibitor of Intestinal Na<sup>+</sup>/H<sup>+</sup> Exchanger Isoform 3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 7.15 | 9.30 |
| pIC50 | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3304485 | TENAPANOR | 4.0 | 1 | 9.30 |
| CHEMBL5176968 | — | — | 1 | 8.90 |
| CHEMBL5170002 | — | — | 1 | 8.80 |
| CHEMBL3990220 | — | — | 1 | 8.80 |
| CHEMBL5202545 | — | — | 1 | 8.70 |
| CHEMBL5183104 | — | — | 1 | 8.40 |
| CHEMBL5170188 | — | — | 1 | 8.10 |
| CHEMBL5202068 | — | — | 1 | 8.10 |
| CHEMBL4289255 | — | — | 1 | 7.60 |
| CHEMBL3906248 | — | — | 1 | 7.50 |
| CHEMBL3908998 | — | — | 1 | 7.40 |
| CHEMBL3984342 | — | — | 1 | 7.40 |
| CHEMBL3950244 | — | — | 1 | 7.30 |
| CHEMBL5172917 | — | — | 1 | 7.30 |
| CHEMBL3971033 | — | — | 1 | 7.20 |
| CHEMBL3963559 | — | — | 1 | 7.20 |
| CHEMBL5207418 | — | — | 1 | 7.20 |
| CHEMBL5200502 | — | — | 1 | 7.10 |
| CHEMBL5190823 | — | — | 1 | 7.00 |
| CHEMBL5189049 | — | — | 1 | 6.80 |
| CHEMBL3901448 | — | — | 1 | 6.70 |
| CHEMBL5182162 | — | — | 1 | 6.70 |
| CHEMBL3986031 | — | — | 1 | 6.50 |
| CHEMBL5198774 | — | — | 1 | 6.50 |
| CHEMBL3964255 | — | — | 1 | 6.30 |
| CHEMBL3890952 | — | — | 1 | 6.20 |
| CHEMBL5193832 | — | — | 1 | 6.00 |
| CHEMBL3932557 | — | — | 1 | 5.80 |
| CHEMBL3918734 | — | — | 1 | 5.70 |
| CHEMBL5202143 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3304485 | TENAPANOR | IC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL5176968 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL3990220 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5170002 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL5202545 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL5183104 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL5170188 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL5202068 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL4289255 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL3906248 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL3908998 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3984342 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL3950244 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5172917 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL5207418 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3971033 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL3963559 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5200502 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL5190823 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5189049 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL3901448 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL5182162 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL5198774 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3986031 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL3964255 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL3890952 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL5193832 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3932557 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3918734 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL5202143 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL5209058 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL5181913 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL3953700 | — | IC50 | > | 3162.28 | nM | - |
| CHEMBL5198507 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL3956290 | — | IC50 | > | 3162.28 | nM | - |
| CHEMBL5194676 | — | pIC50 | - | — | - | |
| CHEMBL3901687 | — | pIC50 | - | — | - | |
| CHEMBL3953181 | — | pIC50 | - | — | - | |
| CHEMBL3902694 | — | pIC50 | - | — | - | |
| CHEMBL3894457 | — | pIC50 | - | — | - | |
| CHEMBL3901018 | — | IC50 | > | 3162.28 | nM | - |
| CHEMBL5193809 | — | pIC50 | - | — | - | |
| CHEMBL3990607 | — | pIC50 | - | — | - | |
| CHEMBL5185356 | — | pIC50 | - | — | - | |
| CHEMBL3991236 | — | pIC50 | - | — | - | |
| CHEMBL3892919 | — | pIC50 | - | — | - |