Assay Detail
Binding
CHEMBL684126
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In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
77
Total Activities
77
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | BHK |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 77 | 7.53 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL152640 | — | — | 1 | 8.64 |
| CHEMBL152477 | — | — | 1 | 8.55 |
| CHEMBL156724 | — | — | 1 | 8.47 |
| CHEMBL348702 | — | — | 1 | 8.37 |
| CHEMBL154159 | — | — | 1 | 8.34 |
| CHEMBL154149 | — | — | 1 | 8.31 |
| CHEMBL153157 | — | — | 1 | 8.28 |
| CHEMBL152293 | — | — | 1 | 8.24 |
| CHEMBL152464 | — | — | 1 | 8.23 |
| CHEMBL152691 | — | — | 1 | 8.21 |
| CHEMBL421809 | — | — | 1 | 8.21 |
| CHEMBL2112908 | — | — | 1 | 8.19 |
| CHEMBL152207 | — | — | 1 | 8.18 |
| CHEMBL2112906 | — | — | 1 | 8.16 |
| CHEMBL2111262 | — | — | 1 | 8.13 |
| CHEMBL154400 | — | — | 1 | 8.13 |
| CHEMBL153641 | — | — | 1 | 8.10 |
| CHEMBL157380 | — | — | 1 | 8.08 |
| CHEMBL155065 | — | — | 1 | 8.08 |
| CHEMBL156904 | — | — | 1 | 8.04 |
| CHEMBL153879 | — | — | 1 | 7.98 |
| CHEMBL152184 | — | — | 1 | 7.95 |
| CHEMBL154316 | — | — | 1 | 7.94 |
| CHEMBL158295 | — | — | 1 | 7.94 |
| CHEMBL346464 | — | — | 1 | 7.91 |
| CHEMBL2111565 | — | — | 1 | 7.89 |
| CHEMBL156772 | — | — | 1 | 7.86 |
| CHEMBL346694 | — | — | 1 | 7.84 |
| CHEMBL153950 | — | — | 1 | 7.83 |
| CHEMBL413964 | — | — | 1 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL152640 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL152477 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL156724 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL348702 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL154159 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL154149 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL153157 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL152293 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL152464 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL152691 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL421809 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL2112908 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL152207 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL2112906 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL154400 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL2111262 | — | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL153641 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL157380 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL155065 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL156904 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL153879 | — | IC50 | = | 10.4 | nM | 7.98 |
| CHEMBL152184 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL154316 | — | IC50 | = | 11.4 | nM | 7.94 |
| CHEMBL158295 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL346464 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL2111565 | — | IC50 | = | 12.9 | nM | 7.89 |
| CHEMBL156772 | — | IC50 | = | 13.8 | nM | 7.86 |
| CHEMBL346694 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL153950 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL413964 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL157280 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL2112907 | — | IC50 | = | 19.1 | nM | 7.72 |
| CHEMBL152409 | — | IC50 | = | 19.7 | nM | 7.71 |
| CHEMBL152765 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2111214 | — | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL345713 | — | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL422506 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL349552 | — | IC50 | = | 22.9 | nM | 7.64 |
| CHEMBL153038 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL359126 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL346801 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL157000 | — | IC50 | = | 28.7 | nM | 7.54 |
| CHEMBL153905 | — | IC50 | = | 29.4 | nM | 7.53 |
| CHEMBL345589 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL352005 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL152103 | — | IC50 | = | 33.5 | nM | 7.47 |
| CHEMBL156666 | — | IC50 | = | 33.8 | nM | 7.47 |
| CHEMBL154460 | — | IC50 | = | 35.4 | nM | 7.45 |
| CHEMBL156837 | — | IC50 | = | 38.8 | nM | 7.41 |
| CHEMBL153438 | — | IC50 | = | 41.1 | nM | 7.39 |