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ChEMBL ligand: CHEMBL310843 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | Inhibition of human dopamine D1 receptor | B | 5.26 | pKi | 5500 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130] | ||||||||
ChEMBL | Binding affinity to pig cortical membrane dopamine D1 receptor | B | 5.26 | pKi | 5500 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 983-988 [PMID:18164618] |
ChEMBL | Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane | B | 5.26 | pKi | 5500 | nM | Ki | J Med Chem (2008) 51: 1800-1810 [PMID:18307287] |
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
ChEMBL | Binding affinity against dopamine receptor D1 using radioligand [3H]-SCH- 23390 | B | 5.26 | pKi | 5500 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2L receptor E181V/I183S mutant expressed in HEK293 cells | B | 4.33 | pKi | 47000 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Displacement of [3H]spiperone from cloned human dopamine D2S receptor expressed in CHO cells | B | 5.2 | pKi | 6300 | nM | Ki | J Med Chem (2008) 51: 1800-1810 [PMID:18307287] |
ChEMBL | Binding affinity against dopamine receptor D2S using radioligand [3H]spiperone | B | 5.2 | pKi | 6300 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | Inhibition of human dopamine D2 (short) receptor | B | 5.2 | pKi | 6300 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
ChEMBL | Inhibition of human dopamine D2 (long) receptor (unknown origin) | B | 5.22 | pKi | >6000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
ChEMBL | Binding affinity to human dopamine D2 long receptor | B | 5.47 | pKi | 3400 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 983-988 [PMID:18164618] |
ChEMBL | Displacement of [3H]spiperone from cloned human dopamine D2L receptor expressed in CHO cells | B | 5.47 | pKi | 3400 | nM | Ki | J Med Chem (2008) 51: 1800-1810 [PMID:18307287] |
ChEMBL | Binding affinity for human dopamine receptor D2 long | B | 5.47 | pKi | 3400 | nM | Ki | J Med Chem (2005) 48: 694-709 [PMID:15689154] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2L receptor expressed in CHO cells | B | 5.47 | pKi | 3400 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Binding affinity against dopamine receptor D2L using radioligand [3H]-spiperone | B | 5.47 | pKi | 3400 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | Binding affinity to dopamine D2 | B | 5.47 | pKi | 3388.44 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D2 receptor | B | 5.49 | pKi | 3200 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5077-5081 [PMID:23920439] |
ChEMBL | Displacement of [3H]spiperone from wild type human cloned dopamine D2L receptor expressed in HEK293 cells | B | 5.64 | pKi | 2300 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Binding affinity against human Dopamine receptor D2 using [3H]spiperone as radioligand | B | 5.88 | pKi | 1310 | nM | Ki | J Med Chem (2004) 47: 2348-2355 [PMID:15084133] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor D3.32E mutant expressed in HEK293 cells | B | 4.92 | pKi | 12000 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F mutant expressed in HEK293 cells | B | 5.04 | pKi | 9200 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Displacement of [3H]spiperone from wild type human cloned dopamine D3 receptor expressed in HEK293 cells | B | 5.08 | pKi | 8300 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Displacement of [3H]spiperone from cloned human dopamine D3 receptor expressed in CHO cells | B | 5.28 | pKi | 5300 | nM | Ki | J Med Chem (2008) 51: 1800-1810 [PMID:18307287] |
ChEMBL | Binding affinity against dopamine receptor D3 using radioligand [3H]spiperone | B | 5.28 | pKi | 5300 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | Binding affinity for human dopamine receptor D3 | B | 5.28 | pKi | 5300 | nM | Ki | J Med Chem (2005) 48: 694-709 [PMID:15689154] |
ChEMBL | Binding affinity to human D3 receptor | B | 5.28 | pKi | 5300 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 983-988 [PMID:18164618] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO cells | B | 5.28 | pKi | 5300 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Inhibition of human dopamine D3 receptor | B | 5.28 | pKi | 5300 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane | B | 5.28 | pKi | 5248.07 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
ChEMBL | Binding affinity to human dopamine D3 receptor by radioligand binding assay | B | 5.3 | pKi | 5000 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5077-5081 [PMID:23920439] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor V180E/S182I mutant expressed in HEK293 cells | B | 5.6 | pKi | 2500 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor L2.64F mutant expressed in HEK293 cells | B | 5.8 | pKi | 1600 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor FV3.28,3.29LM mutant expressed in HEK293 cells | B | 6.14 | pKi | 730 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor V2.61F/FV3.28,3.29LM mutant expressed in HEK293 cells | B | 7.12 | pKi | 76 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D3 receptor H6.55A mutant expressed in HEK293 cells | B | 7.34 | pKi | 46 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Displacement of [3H]spiperone from wild type human cloned dopamine D4 receptor expressed in HEK293 cells | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Binding affinity to human dopamine D4 receptor by radioligand binding assay | B | 8.51 | pKi | 3.1 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5077-5081 [PMID:23920439] |
ChEMBL | Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement. | B | 8.57 | pKi | 2.7 | nM | Ki | J Med Chem (2004) 47: 2348-2355 [PMID:15084133] |
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D4 receptor expressed in CHO cells | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2009) 52: 4923-4935 [PMID:19606869] |
ChEMBL | Binding affinity to human dopamine D4.4 receptor | B | 8.66 | pKi | 2.2 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 983-988 [PMID:18164618] |
ChEMBL | Binding affinity for Dopamine receptor D4 | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2005) 48: 694-709 [PMID:15689154] |
ChEMBL | Binding affinity against human dopamine receptor D4.4 using radioligand [3H]spiperone | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2001) 44: 2691-2694 [PMID:11495580] |
ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane | B | 8.66 | pKi | 2.19 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
ChEMBL | Ability to displace [3H]spiperone from dopamine receptor D4.4 expressed in CHO-K1 cells | B | 8.66 | pKi | 8.66 | D4 | Log Ki | J Med Chem (2001) 44: 1151-1157 [PMID:11312915] |
ChEMBL | Effective concentration against human Dopamine receptor D4 | B | 6.81 | pEC50 | 154 | nM | EC50 | J Med Chem (2004) 47: 2348-2355 [PMID:15084133] |
D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
GtoPdb | - | - | 9 | pKi | - | - | - | Mol Pharmacol (2004) 66: 1491-9 [PMID:15448188] |
GtoPdb | - | - | 9 | pKi | - | - | - | Mol Pharmacol (2004) 66: 1491-9 [PMID:15448188] |
Serotonin 2a (5-HT2a) receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2490] [UniProtKB: P50129] | ||||||||
ChEMBL | Displacement of [3H]ketanserin from pig cortical membrane 5HT2 receptor | B | 6.05 | pKi | 900 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 983-988 [PMID:18164618] |
ChEMBL | Displacement of [3H]ketanserin from 5HT2 receptor in pig cortical membranes | B | 6.05 | pKi | 900 | nM | Ki | J Med Chem (2008) 51: 1800-1810 [PMID:18307287] |
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]