Assay Detail
Binding
CHEMBL4012481
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Inhibition of human CYP11B2 expressed in HEK293A cells using deoxycorticosterone as substrate pretreated for 1 hr followed by substrate addition measured after 1 hr by HTRF assay
25
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
4-Anilino-pyrimidine, novel aldosterone synthase (CYP11B2) inhibitors bearing pyrimidine structures.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.88 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4088766 | — | — | 1 | 9.40 |
| CHEMBL4082403 | — | — | 3 | 9.14 |
| CHEMBL4070323 | — | — | 1 | 8.70 |
| CHEMBL4070230 | — | — | 1 | 8.70 |
| CHEMBL4091167 | — | — | 1 | 8.52 |
| CHEMBL4099824 | — | — | 1 | 8.52 |
| CHEMBL287677 | DEXFADROSTAT | 2.0 | 1 | 8.40 |
| CHEMBL4093575 | — | — | 1 | 8.30 |
| CHEMBL4072943 | — | — | 1 | 8.30 |
| CHEMBL4097020 | — | — | 1 | 8.15 |
| CHEMBL4061565 | — | — | 1 | 8.10 |
| CHEMBL4092081 | — | — | 1 | 8.10 |
| CHEMBL4064367 | — | — | 1 | 7.85 |
| CHEMBL4079006 | — | — | 1 | 7.82 |
| CHEMBL4065476 | — | — | 1 | 7.52 |
| CHEMBL4072871 | — | — | 1 | 7.32 |
| CHEMBL4104118 | — | — | 1 | 7.12 |
| CHEMBL4083387 | — | — | 1 | 7.08 |
| CHEMBL4067686 | — | — | 1 | 6.96 |
| CHEMBL4075207 | — | — | 1 | 6.84 |
| CHEMBL4101118 | — | — | 1 | 6.72 |
| CHEMBL4077051 | — | — | 1 | 6.52 |
| CHEMBL4060559 | — | — | 1 | 6.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4088766 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4082403 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL4070323 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4070230 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4091167 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4099824 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4082403 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL287677 | DEXFADROSTAT | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4072943 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4093575 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4097020 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4061565 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4092081 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4064367 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4079006 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4065476 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4072871 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4104118 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4083387 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4067686 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL4075207 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL4101118 | — | IC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4060559 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4077051 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4082403 | — | IC50 | > | 100.0 | nM | - |