Assay Detail
Functional
CHEMBL652568
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Growth inhibition of CCRF-CEM human leukemic lymphoblasts
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CCRF-CEM |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Analogues of the potent nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523) with modifications in the side chain, p-aminobenzoyl moiety, or 9,10-bridge: synthesis and in vitro antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.43 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL297566 | — | — | 1 | 9.28 |
| CHEMBL298032 | — | — | 1 | 9.20 |
| CHEMBL42141 | — | — | 1 | 8.92 |
| CHEMBL275023 | — | — | 1 | 8.92 |
| CHEMBL18155 | — | — | 1 | 8.82 |
| CHEMBL44919 | — | — | 1 | 8.54 |
| CHEMBL296373 | EDATREXATE | 2.0 | 1 | 8.48 |
| CHEMBL42889 | — | — | 1 | 8.36 |
| CHEMBL376180 | AMINOPTERIN | 2.0 | 1 | 8.36 |
| CHEMBL290590 | — | — | 1 | 8.30 |
| CHEMBL43150 | — | — | 1 | 8.29 |
| CHEMBL42819 | — | — | 1 | 8.26 |
| CHEMBL42142 | — | — | 1 | 8.12 |
| CHEMBL42888 | — | — | 1 | 7.27 |
| CHEMBL42109 | — | — | 1 | 7.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL297566 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL298032 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL42141 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL275023 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL18155 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL44919 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL296373 | EDATREXATE | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL42889 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL376180 | AMINOPTERIN | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL290590 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL43150 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL42819 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL42142 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL42888 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL42109 | — | IC50 | = | 55.0 | nM | 7.26 |