P25098 | ARBK1_HUMAN | Beta-adrenergic receptor kinase 1 (GRK2)
Pfam Domain Table
| Accession | Domain | Range | Color |
|---|---|---|---|
| PF00069 | Pkinase - Protein kinase domain | 192~453 | |
| PF00169 | PH - PH domain | 560~650 | |
| PF00615 | RGS - Regulator of G protein signaling domain | 55~174 |
3D structures mapped by conservation among orthologs
[ Domain: "PH domain-like" // PH ]
[ Domain: "Regulator of G-protein signaling, RGS" // RGS ]
[ Domain: "Protein kinase" // Pkinase_Tyr ]
[ Domain: "Protein kinase" // Pkinase_Tyr,RGS ]
[ Alpha Fold Model ] (go)
Known binders annotated in ChEMBL
| molecule_chembl_id | structure | assay_type | relation | value | unit | mol_wt | smiles | organism | assay_chembl_id | bao_label |
|---|---|---|---|---|---|---|---|---|---|---|
| CHEMBL4073882 |  |
IC50 | = | 1.7 | nM | 462.46 | O=C(NCc1c(F)cccc1F)c1cccc(NCc2nnc3n2CCOc2cnccc2-3)c1 | Homo sapiens | CHEMBL4040375 | assay format |
| CHEMBL4072828 |  |
IC50 | = | 1.8 | nM | 494.48 | O=C(NCc1ccccc1C(F)(F)F)c1cccc(NCc2nnc3n2CCOc2cnccc2-3)c1 | Homo sapiens | CHEMBL4040375 | assay format |
| CHEMBL4086046 |  |
IC50 | = | 1.9 | nM | 495.51 | CCCn1c(CNc2cccc(C(=O)NCc3ccccc3C(F)(F)F)c2)nnc1-c1ccncn1 | Homo sapiens | CHEMBL4040375 | assay format |
| CHEMBL3716385 |  |
IC50 | = | 2.0 | nM | 510.93 | CC(=O)Nc1cc(NC(C)(C)C(=O)Nc2nc3c(C(F)(F)F)cc4[nH]ncc4c3s2)ccc1Cl | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL3718650 |  |
IC50 | = | 2.8 | nM | 442.93 | CC(=O)Nc1cc(NC(C)(C)C(=O)Nc2nc3ccc4[nH]ncc4c3s2)ccc1Cl | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL4095659 |  |
IC50 | = | 3.0 | nM | 414.47 | COc1ccccc1CNC(=O)c1cccc(NCc2nnc(-c3ccncc3)[nH]2)c1 | Homo sapiens | CHEMBL4040375 | assay format |
| CHEMBL3719041 |  |
IC50 | = | 3.2 | nM | 496.9 | CC(C)(Nc1ccc(Cl)c(C(N)=O)c1)C(=O)Nc1nc2c(C(F)(F)F)cc3[nH]ncc3c2s1 | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL3716440 |  |
IC50 | = | 3.2 | nM | 524.96 | CCC(=O)Nc1cc(NC(C)(C)C(=O)Nc2nc3c(C(F)(F)F)cc4[nH]ncc4c3s2)ccc1Cl | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL3718067 |  |
IC50 | = | 3.7 | nM | 424.46 | CC(=O)Nc1cc(NC2(C(=O)Nc3nc4ccc5[nH]ncc5c4s3)CC2)ccc1F | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL4077447 |  |
IC50 | = | 3.9 | nM | 418.89 | O=C(NCc1ccccc1Cl)c1cccc(NCc2nnc(-c3ccncc3)[nH]2)c1 | Homo sapiens | CHEMBL4040375 | assay format |
| CHEMBL3718849 |  |
IC50 | = | 3.9 | nM | 456.96 | CCC(=O)Nc1cc(NC(C)(C)C(=O)Nc2nc3ccc4[nH]ncc4c3s2)ccc1Cl | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL3718984 |  |
IC50 | = | 3.9 | nM | 383.86 | O=C(Nc1nc2ccc3[nH]ncc3c2s1)C1(Nc2ccc(Cl)cc2)CC1 | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL3716298 |  |
IC50 | = | 4.0 | nM | 373.83 | O=C(CNc1ccc(Cl)c(O)c1)Nc1nc2ccc3[nH]ncc3c2s1 | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL3719096 |  |
IC50 | = | 4.5 | nM | 524.96 | CCNC(=O)c1cc(NC(C)(C)C(=O)Nc2nc3c(C(F)(F)F)cc4[nH]ncc4c3s2)ccc1Cl | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL3715310 |  |
IC50 | = | 4.6 | nM | 438.49 | CCC(=O)Nc1cc(NC2(C(=O)Nc3nc4ccc5[nH]ncc5c4s3)CC2)ccc1F | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL4071398 |  |
IC50 | = | 5.5 | nM | 496.49 | O=C(NCc1ccccc1C(F)(F)F)c1cccc(NCc2nnc(-c3ccncc3)n2CCO)c1 | Homo sapiens | CHEMBL4040375 | assay format |
| CHEMBL4742990 |  |
IC50 | = | 6.0 | nM | 332.36 | COc1cccc(Cn2cnc3ccc(-c4cn[nH]c4)cc3c2=O)c1 | Homo sapiens | CHEMBL4703643 | single protein format |
| CHEMBL4082775 |  |
IC50 | = | 6.1 | nM | 384.44 | O=C(NCc1ccccc1)c1cccc(NCc2nc(-c3ccncc3)n[nH]2)c1 | Homo sapiens | CHEMBL4040375 | assay format |
| CHEMBL3714916 |  |
IC50 | = | 6.2 | nM | 397.89 | Cc1cc2[nH]ncc2c2sc(NC(=O)C3(Nc4ccc(Cl)cc4)CC3)nc12 | Homo sapiens | CHEMBL3721218 | cell-based format |
| CHEMBL3717041 |  |
IC50 | = | 6.3 | nM | 510.93 | CNC(=O)c1cc(NC(C)(C)C(=O)Nc2nc3c(C(F)(F)F)cc4[nH]ncc4c3s2)ccc1Cl | Homo sapiens | CHEMBL3721218 | cell-based format |