Assay Detail
Functional
CHEMBL2446560
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
30
Total Activities
18
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of N-alkyl-S-[3-(piperidin-1-yl)propyl]isothioureas: high affinity and human/rat species-selective histamine H(3) receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.32 | 9.10 |
| Kd | 9 | 8.49 | 10.00 |
| pA2 | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | — | 2 | 10.00 |
| CHEMBL2441942 | — | — | 2 | 9.60 |
| CHEMBL2441946 | — | — | 2 | 8.70 |
| CHEMBL2441945 | — | — | 2 | 8.70 |
| CHEMBL2441941 | — | — | 2 | 8.70 |
| CHEMBL2441940 | — | — | 2 | 8.10 |
| CHEMBL2441943 | — | — | 2 | 8.00 |
| CHEMBL2441944 | — | — | 2 | 7.90 |
| CHEMBL2441933 | — | — | 1 | 7.70 |
| CHEMBL2441938 | — | — | 1 | 7.50 |
| CHEMBL2441935 | — | — | 2 | 7.40 |
| CHEMBL2441948 | — | — | 2 | 6.90 |
| CHEMBL2441947 | — | — | 2 | 6.90 |
| CHEMBL2441949 | — | — | 2 | 6.50 |
| CHEMBL2441939 | — | — | 1 | 6.50 |
| CHEMBL2441936 | — | — | 1 | 5.90 |
| CHEMBL2441934 | — | — | 1 | 5.80 |
| CHEMBL2441937 | — | — | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL14690 | CLOBENPROPIT | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL2441942 | — | Kd | = | 0.2512 | nM | 9.60 |
| CHEMBL14690 | CLOBENPROPIT | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL2441945 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL2441946 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL2441945 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL2441941 | — | Kd | = | 1.995 | nM | 8.70 |
| CHEMBL2441946 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL2441941 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL2441942 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL2441940 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL2441943 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL2441944 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL2441944 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL2441933 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL2441943 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL2441938 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL2441940 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL2441935 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL2441935 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL2441948 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL2441947 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL2441949 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL2441939 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL2441936 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL2441934 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL2441937 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL2441949 | — | pA2 | - | — | - | |
| CHEMBL2441948 | — | pA2 | - | — | - | |
| CHEMBL2441947 | — | pA2 | - | — | - |