Assay Detail
Binding
CHEMBL4880047
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GPCRScan assay: inhibition of H2
203
Total Activities
181
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 | 181 | - | - |
| Ki | 22 | 6.00 | 7.67 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | Stable HEK |
| PMID | PMID | - | — | 8961278.0 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 0.02 – 0.05 |
| Radioligand Kd | Radioligand Kd | 0.03 | nM | — |
| Radioligand name | Radioligand name | - | — | [125I]-Iodo-aminopotentidine |
| Radioligand pKd | Radioligand pKd | 10.47 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.12 | — | — |
| Reference ligand | Reference ligand | - | — | ORG-5222 |
| Reference ligand Ki | Reference ligand Ki | 0.9 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 9.05 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.04 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4520788 | BAY-294 | — | 3 | 7.67 |
| CHEMBL4535474 | BAY-293 | — | 3 | 6.86 |
| CHEMBL4748908 | TP-040n | — | 3 | 6.84 |
| CHEMBL4795065 | Borussertib | — | 3 | 6.09 |
| CHEMBL3609749 | — | — | 3 | 6.01 |
| CHEMBL4576555 | T3-CLK-N | — | 3 | 5.79 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.75 |
| CHEMBL5086970 | — | — | 3 | 5.57 |
| CHEMBL4558518 | GSI-NC | — | 3 | 5.42 |
| CHEMBL4448899 | BAY-876 | — | 3 | 5.10 |
| CHEMBL4555711 | BAY-9897 | — | 3 | 5.01 |
| CHEMBL4445670 | BAY-885 | — | 1 | - |
| CHEMBL4552180 | BAY-588 | — | 1 | - |
| CHEMBL4564312 | BAY-786 | — | 1 | - |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4516843 | BAY-207 | — | 1 | - |
| CHEMBL4521594 | BAY-1797 | — | 1 | - |
| CHEMBL4539943 | BAY-694 | — | 1 | - |
| CHEMBL4585243 | BAY-7598 | — | 1 | - |
| CHEMBL4522773 | BAY-827 | — | 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 |
|---|---|---|---|---|---|---|
| CHEMBL4520788 | BAY-294 | Ki | = | 21.13 | nM | 7.67 |
| CHEMBL4520788 | BAY-294 | Ki | = | 21.13 | nM | 7.67 |
| CHEMBL4535474 | BAY-293 | Ki | = | 139.64 | nM | 6.86 |
| CHEMBL4535474 | BAY-293 | Ki | = | 139.82 | nM | 6.85 |
| CHEMBL4748908 | TP-040n | Ki | = | 144.54 | nM | 6.84 |
| CHEMBL4748908 | TP-040n | Ki | = | 148.82 | nM | 6.83 |
| CHEMBL4795065 | Borussertib | Ki | = | 812.83 | nM | 6.09 |
| CHEMBL4795065 | Borussertib | Ki | = | 949.61 | nM | 6.02 |
| CHEMBL3609749 | — | Ki | = | 975.0 | nM | 6.01 |
| CHEMBL3609749 | — | Ki | = | 977.24 | nM | 6.01 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 1621.81 | nM | 5.79 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 1725.74 | nM | 5.76 |
| CHEMBL3480577 | UCSF924 | Ki | = | 1778.28 | nM | 5.75 |
| CHEMBL3480577 | UCSF924 | Ki | = | 1909.67 | nM | 5.72 |
| CHEMBL5086970 | — | Ki | = | 2691.53 | nM | 5.57 |
| CHEMBL5086970 | — | Ki | = | 2960.61 | nM | 5.53 |
| CHEMBL4558518 | GSI-NC | Ki | = | 3794.0 | nM | 5.42 |
| CHEMBL4558518 | GSI-NC | Ki | = | 3801.89 | nM | 5.42 |
| CHEMBL4448899 | BAY-876 | Ki | = | 7943.28 | nM | 5.10 |
| CHEMBL4448899 | BAY-876 | Ki | = | 8078.0 | nM | 5.09 |
| CHEMBL4555711 | BAY-9897 | Ki | = | 9781.38 | nM | 5.01 |
| CHEMBL4555711 | BAY-9897 | Ki | = | 9772.37 | nM | 5.01 |
| CHEMBL4282264 | A-485 | Inhibition | = | 28.24 | % | - |
| CHEMBL4561806 | BTZO-4 | Inhibition | = | 24.76 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 31.91 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | 5.46 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | 0.52 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | 11.93 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | 4.01 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | 29.97 | % | - |
| CHEMBL4580220 | BAY-3827 | Inhibition | = | 12.65 | % | - |
| CHEMBL4228713 | A-1211212 | Inhibition | = | 13.55 | % | - |
| CHEMBL4538591 | BAY-440 | Inhibition | = | 32.65 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 23.28 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | 8.7 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | 5.32 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | 6.93 | % | - |
| CHEMBL4798829 | — | Inhibition | = | 14.82 | % | - |
| CHEMBL4545807 | BAY-070 | Inhibition | = | 1.91 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | 12.29 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | -3.94 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | 4.49 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 11.73 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | 3.1 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | 3.0 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | 15.69 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | 11.84 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | 10.99 | % | - |
| CHEMBL3137331 | DEFACTINIB | Inhibition | = | 30.19 | % | - |
| CHEMBL4647642 | BAY-173 | Inhibition | = | 8.13 | % | - |