Assay Detail
Binding
CHEMBL4880049
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GPCRScan assay: inhibition of H4
193
Total Activities
179
Compounds Tested
2
Activity Types
12
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
SGC PDSP GPCRScan assays
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 179 | - | - |
| Ki | 14 | 5.68 | 6.16 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | HEK T |
| PMID | PMID | - | — | 16432504/11561071 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 1.0 – 5.0 |
| Radioligand Kd | Radioligand Kd | 5.46 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-Histamine |
| Radioligand pKd | Radioligand pKd | 8.26 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.08 | — | — |
| Reference ligand | Reference ligand | - | — | Clozapine |
| Reference ligand Ki | Reference ligand Ki | 250.0 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 6.6 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.06 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748908 | TP-040n | — | 5 | 6.16 |
| CHEMBL1834199 | BI 99990 | — | 3 | 5.80 |
| CHEMBL4520788 | BAY-294 | — | 3 | 5.72 |
| CHEMBL3623630 | — | — | 3 | 5.47 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.00 |
| CHEMBL4552554 | PF-04475866 | — | 3 | 5.00 |
| CHEMBL4521594 | BAY-1797 | — | 1 | - |
| CHEMBL4096813 | — | — | 1 | - |
| CHEMBL4516843 | BAY-207 | — | 1 | - |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4564312 | BAY-786 | — | 1 | - |
| CHEMBL4448899 | BAY-876 | — | 1 | - |
| CHEMBL4552180 | BAY-588 | — | 1 | - |
| CHEMBL4445670 | BAY-885 | — | 1 | - |
| CHEMBL4455582 | BAY-693 | — | 1 | - |
| CHEMBL4630644 | BAY-386 | — | 1 | - |
| CHEMBL4630643 | BAY-448 | — | 1 | - |
| CHEMBL3907057 | BAY-826 | — | 1 | - |
| CHEMBL4539943 | BAY-694 | — | 1 | - |
| CHEMBL4585243 | BAY-7598 | — | 1 | - |
| CHEMBL4593677 | BAY-474 | — | 1 | - |
| CHEMBL4066040 | A-1596584 | — | 1 | - |
| CHEMBL4093612 | A-1596586 | — | 1 | - |
| CHEMBL332794 | A-192621 | — | 1 | - |
| CHEMBL4513786 | A-545 | — | 1 | - |
| CHEMBL111612 | ABT-546 | — | 1 | - |
| CHEMBL4526341 | A-108 | — | 1 | - |
| CHEMBL4586794 | ABT-100 | — | 1 | - |
| CHEMBL3701197 | A-226 | — | 1 | - |
| CHEMBL3697701 | A-079 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4748908 | TP-040n | Ki | = | 691.83 | nM | 6.16 |
| CHEMBL4748908 | TP-040n | Ki | = | 703.07 | nM | 6.15 |
| CHEMBL4748908 | TP-040n | Ki | = | 711.87 | nM | 6.15 |
| CHEMBL4748908 | TP-040n | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL1834199 | BI 99990 | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL1834199 | BI 99990 | Ki | = | 1635.0 | nM | 5.79 |
| CHEMBL4520788 | BAY-294 | Ki | = | 1905.46 | nM | 5.72 |
| CHEMBL4520788 | BAY-294 | Ki | = | 1885.82 | nM | 5.72 |
| CHEMBL3623630 | — | Ki | = | 3382.0 | nM | 5.47 |
| CHEMBL4552554 | PF-04475866 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4552554 | PF-04475866 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL3480577 | UCSF924 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4538591 | BAY-440 | Inhibition | = | -2.29 | % | - |
| CHEMBL4555711 | BAY-9897 | Inhibition | = | -17.92 | % | - |
| CHEMBL4580220 | BAY-3827 | Inhibition | = | -10.83 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | -12.98 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | -2.44 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 7.75 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | 12.38 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | -9.05 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | 6.09 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | 14.73 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | -6.41 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 13.11 | % | - |
| CHEMBL4638406 | BAY-3153 | Inhibition | = | -13.92 | % | - |
| CHEMBL4561806 | BTZO-4 | Inhibition | = | 1.885 | % | - |
| CHEMBL4516611 | BTZO-1 | Inhibition | = | -0.9754 | % | - |
| CHEMBL4063249 | TP-021n | Inhibition | = | 4.43 | % | - |
| CHEMBL4075278 | — | Inhibition | = | 11.59 | % | - |
| CHEMBL4647642 | BAY-173 | Inhibition | = | -3.31 | % | - |
| CHEMBL4635540 | GSK791 | Inhibition | = | -23.9 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | -13.53 | % | - |
| CHEMBL4584981 | NVS-MALT1-C | Inhibition | = | -8.46 | % | - |
| CHEMBL4537673 | BAY-985 | Inhibition | = | -0.75 | % | - |
| CHEMBL4568735 | NVS-MALT1 | Inhibition | = | 3.84 | % | - |
| CHEMBL4518706 | PF-00911705 | Inhibition | = | -22.64 | % | - |
| CHEMBL3137331 | DEFACTINIB | Inhibition | = | -19.63 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | 27.64 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | 9.55 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | -26.19 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | -17.71 | % | - |
| CHEMBL3589752 | IPP/CNRS-A017 | Inhibition | = | 3.33 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -11.4 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | -13.26 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | 9.36 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | 29.26 | % | - |
| CHEMBL4545807 | BAY-070 | Inhibition | = | -9.17 | % | - |
| CHEMBL4798829 | — | Inhibition | = | 2.33 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | 5.16 | % | - |
| CHEMBL4514203 | BAY-390 | Inhibition | = | 15.63 | % | - |