Assay Detail
Binding
CHEMBL3118705
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cell membranes preincubated for 30 mins followed by radioligand addition measured after 2 hrs by liquid scintillation counting
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | SK-N-MC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Calcitonin gene-related peptide type 1 receptor (CHEMBL3798) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 50 | 7.80 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL207197 | OLCEGEPANT | 2.0 | 1 | 11.00 |
| CHEMBL3114495 | — | — | 1 | 10.70 |
| CHEMBL3114676 | — | — | 1 | 10.52 |
| CHEMBL3114494 | — | — | 1 | 10.15 |
| CHEMBL3114496 | — | — | 1 | 10.00 |
| CHEMBL3114490 | — | — | 1 | 9.30 |
| CHEMBL3114486 | — | — | 1 | 9.05 |
| CHEMBL3114677 | — | — | 1 | 9.00 |
| CHEMBL3114493 | — | — | 1 | 9.00 |
| CHEMBL3114489 | — | — | 1 | 9.00 |
| CHEMBL3114488 | — | — | 1 | 8.70 |
| CHEMBL3114474 | — | — | 1 | 8.70 |
| CHEMBL3114476 | — | — | 1 | 8.70 |
| CHEMBL3114484 | — | — | 1 | 8.70 |
| CHEMBL3114482 | — | — | 1 | 8.52 |
| CHEMBL3114478 | — | — | 1 | 8.15 |
| CHEMBL3114483 | — | — | 1 | 8.10 |
| CHEMBL3114465 | — | — | 1 | 8.05 |
| CHEMBL3114485 | — | — | 1 | 8.00 |
| CHEMBL3114491 | — | — | 1 | 7.85 |
| CHEMBL3114492 | — | — | 1 | 7.85 |
| CHEMBL3114477 | — | — | 1 | 7.75 |
| CHEMBL3114481 | — | — | 1 | 7.70 |
| CHEMBL3114480 | — | — | 1 | 7.66 |
| CHEMBL3114472 | — | — | 1 | 7.52 |
| CHEMBL3114457 | — | — | 1 | 7.50 |
| CHEMBL3114679 | — | — | 1 | 7.50 |
| CHEMBL3114479 | — | — | 1 | 7.40 |
| CHEMBL3114455 | — | — | 1 | 7.35 |
| CHEMBL3114475 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL207197 | OLCEGEPANT | Ki | = | 0.01 | nM | 11.00 |
| CHEMBL3114495 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL3114676 | — | Ki | = | 0.03 | nM | 10.52 |
| CHEMBL3114494 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL3114496 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL3114490 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3114486 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3114677 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3114493 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3114489 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3114488 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3114474 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3114476 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3114484 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3114482 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL3114478 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL3114483 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL3114465 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL3114485 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3114491 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3114492 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL3114477 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3114481 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL3114480 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3114472 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL3114457 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL3114679 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL3114479 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL3114455 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL3114475 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL3114470 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL3114467 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL3114473 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL3114456 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL3114464 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL3114463 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL3114681 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL3114471 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL3114460 | — | Ki | = | 124.0 | nM | 6.91 |
| CHEMBL3114469 | — | Ki | = | 202.0 | nM | 6.70 |
| CHEMBL3114680 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL3114468 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL3114678 | — | Ki | = | 282.0 | nM | 6.55 |
| CHEMBL3114462 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL3114461 | — | Ki | = | 303.0 | nM | 6.52 |
| CHEMBL3114459 | — | Ki | = | 763.0 | nM | 6.12 |
| CHEMBL3114466 | — | Ki | = | 806.0 | nM | 6.09 |
| CHEMBL3114454 | — | Ki | = | 865.0 | nM | 6.06 |
| CHEMBL3114487 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL3114458 | — | Ki | = | 1880.0 | nM | 5.73 |