FAUC213 [Ligand Id: 974] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL310843
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729]
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  • Serotonin 2a (5-HT2a) receptor in Pig [ChEMBL: CHEMBL2490] [UniProtKB: P50129]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]