Assay Detail
Binding
CHEMBL3788970
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Inhibition of telomerase in human MGC-803 cells after 24 hrs by TRAP-PCR-ELISA assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MGC-803 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Dihydropyrazole derivatives as telomerase inhibitors: Structure-based design, synthesis, SAR and anticancer evaluation in vitro and in vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 42 | 5.15 | 6.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3786231 | — | — | 1 | 6.01 |
| CHEMBL3786261 | — | — | 1 | 5.90 |
| CHEMBL3785281 | — | — | 1 | 5.68 |
| CHEMBL3787380 | — | — | 1 | 5.67 |
| CHEMBL3786734 | — | — | 1 | 5.64 |
| CHEMBL3786296 | — | — | 1 | 5.52 |
| CHEMBL3781973 | — | — | 1 | 5.50 |
| CHEMBL3787157 | — | — | 1 | 5.50 |
| CHEMBL3787509 | — | — | 1 | 5.50 |
| CHEMBL3785699 | — | — | 1 | 5.48 |
| CHEMBL3785712 | — | — | 1 | 5.46 |
| CHEMBL3786636 | — | — | 1 | 5.45 |
| CHEMBL3787476 | — | — | 1 | 5.45 |
| CHEMBL3785112 | — | — | 1 | 5.44 |
| CHEMBL3785686 | — | — | 1 | 5.43 |
| CHEMBL3787002 | — | — | 1 | 5.33 |
| CHEMBL3785474 | — | — | 1 | 5.32 |
| CHEMBL3785170 | — | — | 1 | 5.26 |
| CHEMBL3785833 | — | — | 1 | 5.25 |
| CHEMBL3785907 | — | — | 1 | 5.25 |
| CHEMBL3785758 | — | — | 1 | 5.21 |
| CHEMBL3786451 | — | — | 1 | 5.20 |
| CHEMBL3785664 | — | — | 1 | 5.17 |
| CHEMBL3786821 | — | — | 1 | 5.17 |
| CHEMBL3785794 | — | — | 1 | 5.08 |
| CHEMBL3785970 | — | — | 1 | 5.06 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 5.05 |
| CHEMBL3786236 | — | — | 1 | 5.03 |
| CHEMBL3787163 | — | — | 1 | 5.00 |
| CHEMBL3785883 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3786231 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL3786261 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL3785281 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3787380 | — | IC50 | = | 2120.0 | nM | 5.67 |
| CHEMBL3786734 | — | IC50 | = | 2270.0 | nM | 5.64 |
| CHEMBL3786296 | — | IC50 | = | 3030.0 | nM | 5.52 |
| CHEMBL3781973 | — | IC50 | = | 3170.0 | nM | 5.50 |
| CHEMBL3787157 | — | IC50 | = | 3170.0 | nM | 5.50 |
| CHEMBL3787509 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL3785699 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3785712 | — | IC50 | = | 3440.0 | nM | 5.46 |
| CHEMBL3787476 | — | IC50 | = | 3540.0 | nM | 5.45 |
| CHEMBL3786636 | — | IC50 | = | 3520.0 | nM | 5.45 |
| CHEMBL3785112 | — | IC50 | = | 3630.0 | nM | 5.44 |
| CHEMBL3785686 | — | IC50 | = | 3680.0 | nM | 5.43 |
| CHEMBL3787002 | — | IC50 | = | 4630.0 | nM | 5.33 |
| CHEMBL3785474 | — | IC50 | = | 4770.0 | nM | 5.32 |
| CHEMBL3785170 | — | IC50 | = | 5440.0 | nM | 5.26 |
| CHEMBL3785833 | — | IC50 | = | 5690.0 | nM | 5.25 |
| CHEMBL3785907 | — | IC50 | = | 5570.0 | nM | 5.25 |
| CHEMBL3785758 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL3786451 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL3786821 | — | IC50 | = | 6680.0 | nM | 5.17 |
| CHEMBL3785664 | — | IC50 | = | 6770.0 | nM | 5.17 |
| CHEMBL3785794 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL3785970 | — | IC50 | = | 8740.0 | nM | 5.06 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 8970.0 | nM | 5.05 |
| CHEMBL3786236 | — | IC50 | = | 9320.0 | nM | 5.03 |
| CHEMBL3787163 | — | IC50 | = | 9940.0 | nM | 5.00 |
| CHEMBL3785883 | — | IC50 | = | 10970.0 | nM | 4.96 |
| CHEMBL3787256 | — | IC50 | = | 11030.0 | nM | 4.96 |
| CHEMBL3785132 | — | IC50 | = | 11850.0 | nM | 4.93 |
| CHEMBL3786130 | — | IC50 | = | 13100.0 | nM | 4.88 |
| CHEMBL3786450 | — | IC50 | = | 14250.0 | nM | 4.85 |
| CHEMBL3785623 | — | IC50 | = | 18150.0 | nM | 4.74 |
| CHEMBL3785297 | — | IC50 | = | 22250.0 | nM | 4.65 |
| CHEMBL3787196 | — | IC50 | = | 31210.0 | nM | 4.51 |
| CHEMBL3786403 | — | IC50 | = | 31270.0 | nM | 4.50 |
| CHEMBL3785101 | — | IC50 | = | 35720.0 | nM | 4.45 |
| CHEMBL3787080 | — | IC50 | = | 41180.0 | nM | 4.38 |
| CHEMBL3787238 | — | IC50 | = | 54360.0 | nM | 4.26 |
| CHEMBL3786111 | — | IC50 | = | 57790.0 | nM | 4.24 |