SB 649915 [Ligand Id: 76] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL183460 (SB-649915) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Binding affinity at adrenergic beta 1 receptor | B | 5.6 | pKi | 2511.89 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Negative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptor | B | 6.3 | pKi | <501.19 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [125I]iodosulpiride from human cloned D2 receptor expressed in CHO cells | B | 5.9 | pKi | 1258.93 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [125I]iodosulpiride from human cloned D3 receptor expressed in CHO cells | B | 6.2 | pKi | 630.96 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Displacement of [3H]WAY 100635 from human recombinant 5HT1A receptor expressed in CHO cells | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5214-5217 [PMID:17629698] |
| ChEMBL | Displacement of [3H]WAY-100635 from human cloned 5HT1A receptor expressed in CHO cells | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| ChEMBL | Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | Displacement of [3H]5HT from human cloned 5HT1A receptor expressed in CHO cells | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5581-5585 [PMID:18829312] |
| ChEMBL | Displacement of [3H]WAY-100635 from human 5-hydroxytryptamine 1A receptor expressed in CHO cells | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (2005) 48: 3478-3480 [PMID:15887956] |
| GtoPdb | - | - | 8.6 | pKi | - | - | - | J Med Chem (2005) 48: 3478-80 [PMID:15887956] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells | B | 9.5 | pKi | 0.32 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5214-5217 [PMID:17629698] |
| ChEMBL | Negative logarithm causing 50% receptor occupancy against 5-hydroxytryptamine 1A receptor | B | 9.5 | pKi | 0.32 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| ChEMBL | Mean negative logarithim of binding affinity was measured for the human 5-hydroxytryptamine 1A receptor; n>/=3 | B | 9.5 | pKi | 0.32 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 737-741 [PMID:15664848] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor | B | 9.5 | pKi | 0.32 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| GtoPdb | - | - | 8 | pKi | - | - | - | J Med Chem (2005) 48: 3478-80 [PMID:15887956] |
| ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2005) 48: 3478-3480 [PMID:15887956] |
| ChEMBL | Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| ChEMBL | Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5214-5217 [PMID:17629698] |
| ChEMBL | Displacement of [3H]5HT from human recombinant 5HT1B receptor | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5581-5585 [PMID:18829312] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells | B | 8.8 | pKi | 1.58 | nM | Ki | J Med Chem (2005) 48: 3478-3480 [PMID:15887956] |
| ChEMBL | Displacement of [3H]5-HT from human cloned 5HT1D receptor expressed in CHO cells | B | 8.8 | pKi | 1.58 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| ChEMBL | Displacement of [3H]5-HT from human recombinant 5HT1D receptor expressed in CHO cells | B | 8.8 | pKi | 1.58 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5214-5217 [PMID:17629698] |
| ChEMBL | Displacement of [3H]5HT from human recombinant 5HT1D receptor | B | 8.8 | pKi | 1.58 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | Displacement of [3H]5HT from human cloned 5HT1D receptor expressed in CHO cells | B | 8.8 | pKi | 1.58 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5581-5585 [PMID:18829312] |
| GtoPdb | - | - | 8.8 | pKi | - | - | - | J Med Chem (2005) 48: 3478-80 [PMID:15887956] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from human cloned 5HT2A receptor expressed in HEK293 cells | B | 5.5 | pKi | 3162.28 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells | B | 5.8 | pKi | 1584.89 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]mesulergine from human cloned 5HT2C receptor expressed in HEK293 cells | B | 5.1 | pKi | <7943.28 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells | B | 5 | pKi | <10000 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Displacement of [3H]5CT from human cloned 5HT7a receptor expressed in HEK293 cells | B | 6.7 | pKi | 199.53 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Negative logarithm causing 50% receptor occupancy against serotonin transporter | B | 8.2 | pKi | 6.31 | nM | Ki | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Inhibition of [3H]5-HT uptake at SERT in rat cortical synaptosomes | B | 8 | pKi | 10 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 5214-5217 [PMID:17629698] |
| ChEMBL | Inhibition of [3H]5HT uptake at SERT in rat cortical synaptosomes | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2008) 51: 2887-2890 [PMID:18433113] |
| ChEMBL | Inhibition of [3H]5-HT uptake at SERT in rat cortical synaptosomes | B | 8.1 | pKi | 7.94 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 1033-1036 [PMID:17129726] |
| ChEMBL | Inhibition of [3H]5HT reuptake at SERT in rat cortical synaptosomes | B | 8.1 | pKi | 7.94 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5581-5585 [PMID:18829312] |
| ChEMBL | Mean negative logarithim of binding affinity was measured for the rat serotonin transporter; n>/=3 | B | 8.2 | pKi | 6.31 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 737-741 [PMID:15664848] |
| ChEMBL | Inhibition of [3H]5-HT binding to serotonin transporter in rat cortical synaptosomes | B | 8.4 | pKi | 3.98 | nM | Ki | J Med Chem (2005) 48: 3478-3480 [PMID:15887956] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
