Assay Detail
Functional
CHEMBL835225
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Inhibitory concentration against KBH5.0 cells overexpress BCRP
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KBH5.0 cell |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: variation of n-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.47 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191958 | GENZ-644282 | 1.0 | 1 | 9.30 |
| CHEMBL363839 | — | — | 1 | 8.40 |
| CHEMBL192411 | — | — | 1 | 8.40 |
| CHEMBL177804 | — | — | 1 | 8.30 |
| CHEMBL363340 | — | — | 1 | 8.30 |
| CHEMBL195107 | — | — | 1 | 8.22 |
| CHEMBL195377 | — | — | 1 | 8.22 |
| CHEMBL70790 | — | — | 1 | 8.22 |
| CHEMBL540712 | — | — | 1 | 8.10 |
| CHEMBL195332 | — | — | 1 | 8.05 |
| CHEMBL191032 | — | — | 1 | 8.00 |
| CHEMBL195805 | — | — | 1 | 7.92 |
| CHEMBL191909 | — | — | 1 | 7.40 |
| CHEMBL191245 | — | — | 1 | 7.40 |
| CHEMBL370251 | — | — | 1 | 6.82 |
| CHEMBL195148 | — | — | 1 | 6.52 |
| CHEMBL427002 | — | — | 1 | 6.48 |
| CHEMBL195102 | — | — | 1 | 6.40 |
| CHEMBL84 | TOPOTECAN | 4.0 | 1 | 6.36 |
| CHEMBL195611 | — | — | 1 | 6.30 |
| CHEMBL192202 | — | — | 1 | 6.30 |
| CHEMBL195792 | — | — | 1 | 6.28 |
| CHEMBL194932 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191958 | GENZ-644282 | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL363839 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL192411 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL177804 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL363340 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL195107 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL195377 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL70790 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL540712 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL195332 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL191032 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL195805 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL191909 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL191245 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL370251 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL195148 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL427002 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL195102 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL84 | TOPOTECAN | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL195611 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL192202 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL195792 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL194932 | — | IC50 | = | 750.0 | nM | 6.12 |