PD168,077 [Ligand Id: 975] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL45244 (PD-168077) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276] | ||||||||
| ChEMBL | Binding affinity at Alpha-2 adrenergic receptor | B | 6.75 | pKi | 177 | nM | Ki | J Med Chem (1997) 40: 1771-1772 [PMID:9191952] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL327] [GtoPdb: 25] [UniProtKB: P22909] | ||||||||
| ChEMBL | Binding affinity at alpha-1 adrenergic receptor | B | 6.77 | pKi | 168 | nM | Ki | J Med Chem (1997) 40: 1771-1772 [PMID:9191952] |
| Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
| ChEMBL | Affinity for Dopamine receptor D1 using [3H]SCH-23390 was carried out on bovine retinal membrane preparations | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 161-168 [PMID:12502370] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity for human Dopamine receptor D2 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand | B | 5.43 | pKi | 3740 | nM | Ki | J Med Chem (1997) 40: 1771-1772 [PMID:9191952] |
| ChEMBL | Binding affinity towards cloned human Dopamine receptor D2 | B | 5.43 | pKi | 3740 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 223-226 [PMID:11206464] |
| ChEMBL | Binding affinity towards human dopamine receptor D2 was determined by using [3H]spiperone as radioligand | B | 5.55 | pKi | 2818.38 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2149-2157 [PMID:15808487] |
| ChEMBL | Displacement of [3H] Spiperone from human D2L receptor expressed in CHO cells by competitive radioligand binding assay | B | 5.64 | pKi | 2300 | nM | Ki | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Displacement of [3H] Spiperone from human D2S receptor expressed in CHO cells by competitive radioligand binding assay | B | 5.96 | pKi | 1100 | nM | Ki | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Antagonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 5093-5109 [PMID:16913699] |
| ChEMBL | Agonist activity at human recombinant D2 receptor expressed in HEK293 cells by FLIPR assay | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2006) 49: 5093-5109 [PMID:16913699] |
| Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
| ChEMBL | Affinity for Dopamine receptor D2 using [3H]-YM-09151-2 was carried out on bovine striatal membrane preparations | B | 4.74 | pKi | 18300 | nM | Ki | J Med Chem (2003) 46: 161-168 [PMID:12502370] |
| ChEMBL | Affinity for Dopamine receptor D2 using [3H]YM-09151-2 was carried out on bovine retinal membrane preparations (low-affinity) | B | 5.2 | pKi | 6300 | nM | Ki | J Med Chem (2003) 46: 161-168 [PMID:12502370] |
| ChEMBL | Affinity for Dopamine receptor D2 using [3H]YM-09151-2 was carried out on bovine retinal membrane preparations (high-affinity) | B | 7.6 | pKi | 25 | nM | Ki | J Med Chem (2003) 46: 161-168 [PMID:12502370] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H] Spiperone from human D3 receptor expressed in CHO cells by competitive radioligand binding assay | B | 5.33 | pKi | 4700 | nM | Ki | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Binding affinity for human Dopamine receptor D3 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand | B | 5.55 | pKi | 2810 | nM | Ki | J Med Chem (1997) 40: 1771-1772 [PMID:9191952] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Binding affinity towards human dopamine receptor D4 expressed in CHO cells was determined by using [3H]thymidine as radioligand | B | 7.77 | pKi | 16.98 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2149-2157 [PMID:15808487] |
| ChEMBL | Binding affinity towards cloned human Dopamine receptor D4 | B | 8.05 | pKi | 9 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 223-226 [PMID:11206464] |
| ChEMBL | Binding affinity of compound towards human dopamine receptor D4 was determined | B | 8.06 | pKi | 8.71 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2149-2157 [PMID:15808487] |
| ChEMBL | Binding affinity for human Dopamine receptor D4 expressed in CHO K1 transfected cells using [3H]spiperone as radioligand | B | 8.06 | pKi | 8.7 | nM | Ki | J Med Chem (1997) 40: 1771-1772 [PMID:9191952] |
| ChEMBL | Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Agonist activation of human dopamine receptor stimulating mitogenesis in Dopamine receptor D4-transfected CHO pro-5 cells using [3H]thymidine as radioligand | F | 7.77 | pEC50 | 17 | nM | EC50 | J Med Chem (1997) 40: 1771-1772 [PMID:9191952] |
| ChEMBL | Activity at human recombinant D4.4 receptor expressed in HEK293 cells by FLIPR assay | F | 8.08 | pEC50 | 8.3 | nM | EC50 | J Med Chem (2006) 49: 5093-5109 [PMID:16913699] |
| ChEMBL | Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 8.08 | pEC50 | 8.3 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| GtoPdb | - | - | 8.8 | pKi | 1.58 | nM | Ki | Mol Pharmacol (2004) 66: 1491-9 [PMID:15448188] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264] | ||||||||
| ChEMBL | Binding affinity at 5-hydroxytryptamine 1A receptor | B | 6.41 | pKi | 385 | nM | Ki | J Med Chem (1997) 40: 1771-1772 [PMID:9191952] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity at 5-hydroxytryptamine 2A receptor | B | 5.4 | pKi | 4010 | nM | Ki | J Med Chem (1997) 40: 1771-1772 [PMID:9191952] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
