Assay Detail
Binding
CHEMBL1006149
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Channel opening activity at SUR2B/Kir6.2 potassium ATP channel in human TE671 cells assessed as isometric force by FLIPR
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | TE-671 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
ATP-binding cassette sub-family C member 9 (CHEMBL1971) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and structure-activity relationships of a novel series of benzopyran-based K(ATP) openers for urge urinary incontinence.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 56 | 5.49 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL455408 | — | — | 1 | 7.16 |
| CHEMBL455407 | — | — | 1 | 6.92 |
| CHEMBL11458 | — | — | 1 | 6.64 |
| CHEMBL454369 | — | — | 1 | 6.51 |
| CHEMBL454168 | — | — | 1 | 6.25 |
| CHEMBL473744 | — | — | 1 | 6.17 |
| CHEMBL473941 | — | — | 1 | 6.12 |
| CHEMBL508050 | — | — | 1 | 6.11 |
| CHEMBL454166 | — | — | 1 | 6.09 |
| CHEMBL491479 | — | — | 1 | 6.09 |
| CHEMBL523312 | — | — | 1 | 5.97 |
| CHEMBL49035 | CROMAKALIM | 2.0 | 1 | 5.90 |
| CHEMBL514782 | — | — | 1 | 5.86 |
| CHEMBL462143 | — | — | 1 | 5.82 |
| CHEMBL514789 | — | — | 1 | 5.81 |
| CHEMBL454169 | — | — | 1 | 5.81 |
| CHEMBL517878 | — | — | 1 | 5.79 |
| CHEMBL491471 | — | — | 1 | 5.77 |
| CHEMBL509950 | — | — | 1 | 5.68 |
| CHEMBL490683 | — | — | 1 | 5.64 |
| CHEMBL516207 | — | — | 1 | 5.61 |
| CHEMBL524131 | — | — | 1 | 5.58 |
| CHEMBL449849 | — | — | 1 | 5.56 |
| CHEMBL454398 | — | — | 1 | 5.51 |
| CHEMBL491472 | — | — | 1 | 5.50 |
| CHEMBL1159 | PINACIDIL ANHYDROUS | 4.0 | 1 | 5.45 |
| CHEMBL516977 | — | — | 1 | 5.43 |
| CHEMBL473540 | — | — | 1 | 5.39 |
| CHEMBL460739 | — | — | 1 | 5.36 |
| CHEMBL521608 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL455408 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL455407 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL11458 | — | EC50 | = | 230.0 | nM | 6.64 |
| CHEMBL454369 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL454168 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL473744 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL473941 | — | EC50 | = | 750.0 | nM | 6.12 |
| CHEMBL508050 | — | EC50 | = | 780.0 | nM | 6.11 |
| CHEMBL454166 | — | EC50 | = | 810.0 | nM | 6.09 |
| CHEMBL491479 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL523312 | — | EC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL49035 | CROMAKALIM | EC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL514782 | — | EC50 | = | 1370.0 | nM | 5.86 |
| CHEMBL462143 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL454169 | — | EC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL514789 | — | EC50 | = | 1560.0 | nM | 5.81 |
| CHEMBL517878 | — | EC50 | = | 1640.0 | nM | 5.79 |
| CHEMBL491471 | — | EC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL509950 | — | EC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL490683 | — | EC50 | = | 2290.0 | nM | 5.64 |
| CHEMBL516207 | — | EC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL524131 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL449849 | — | EC50 | = | 2750.0 | nM | 5.56 |
| CHEMBL454398 | — | EC50 | = | 3090.0 | nM | 5.51 |
| CHEMBL491472 | — | EC50 | = | 3160.0 | nM | 5.50 |
| CHEMBL1159 | PINACIDIL ANHYDROUS | EC50 | = | 3540.0 | nM | 5.45 |
| CHEMBL516977 | — | EC50 | = | 3710.0 | nM | 5.43 |
| CHEMBL473540 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL460739 | — | EC50 | = | 4330.0 | nM | 5.36 |
| CHEMBL521608 | — | EC50 | = | 6040.0 | nM | 5.22 |
| CHEMBL517879 | — | EC50 | = | 6180.0 | nM | 5.21 |
| CHEMBL492076 | — | EC50 | = | 6450.0 | nM | 5.19 |
| CHEMBL452140 | — | EC50 | = | 6850.0 | nM | 5.16 |
| CHEMBL513987 | — | EC50 | = | 6940.0 | nM | 5.16 |
| CHEMBL508490 | — | EC50 | = | 7060.0 | nM | 5.15 |
| CHEMBL491281 | — | EC50 | = | 7330.0 | nM | 5.13 |
| CHEMBL461799 | — | EC50 | = | 7450.0 | nM | 5.13 |
| CHEMBL473749 | — | EC50 | = | 7770.0 | nM | 5.11 |
| CHEMBL462140 | — | EC50 | = | 7850.0 | nM | 5.11 |
| CHEMBL523142 | — | EC50 | = | 7990.0 | nM | 5.10 |
| CHEMBL490883 | — | EC50 | = | 8440.0 | nM | 5.07 |
| CHEMBL491674 | — | EC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL460738 | — | EC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL517128 | — | EC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL460911 | — | EC50 | = | 13800.0 | nM | 4.86 |
| CHEMBL515715 | — | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL517594 | — | EC50 | = | 14700.0 | nM | 4.83 |
| CHEMBL460740 | — | EC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL510637 | — | EC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL508720 | — | EC50 | = | 18600.0 | nM | 4.73 |