Assay Detail
Binding
CHEMBL3134683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Jurkat |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Novel FK506 and FK520 analogues via mutasynthesis: mutasynthon scope and product characteristics
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 9.76 | 10.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL269732 | TACROLIMUS ANHYDROUS | 4.0 | 1 | 10.25 |
| CHEMBL3133264 | — | — | 1 | 10.14 |
| CHEMBL3133263 | — | — | 1 | 10.09 |
| CHEMBL3133260 | — | — | 1 | 9.84 |
| CHEMBL8597 | ASCOMYCIN | — | 1 | 9.69 |
| CHEMBL3133261 | — | — | 1 | 9.60 |
| CHEMBL3133266 | — | — | 1 | 9.55 |
| CHEMBL3133262 | — | — | 1 | 9.36 |
| CHEMBL3133265 | — | — | 1 | 9.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL269732 | TACROLIMUS ANHYDROUS | IC50 | = | 0.056 | nM | 10.25 |
| CHEMBL3133264 | — | IC50 | = | 0.072 | nM | 10.14 |
| CHEMBL3133263 | — | IC50 | = | 0.082 | nM | 10.09 |
| CHEMBL3133260 | — | IC50 | = | 0.145 | nM | 9.84 |
| CHEMBL8597 | ASCOMYCIN | IC50 | = | 0.205 | nM | 9.69 |
| CHEMBL3133261 | — | IC50 | = | 0.249 | nM | 9.60 |
| CHEMBL3133266 | — | IC50 | = | 0.283 | nM | 9.55 |
| CHEMBL3133262 | — | IC50 | = | 0.433 | nM | 9.36 |
| CHEMBL3133265 | — | IC50 | = | 0.461 | nM | 9.34 |