FAUC213 [Ligand Id: 974] 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: CHEMBL310843 |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| 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 | 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 | 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 | 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 D2R assessed as inhibition constant | B | 5.47 | pKi | 3400 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| 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 | 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 | 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 | Binding affinity to human D3R assessed as inhibition constant | B | 5.28 | pKi | 5300 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| 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 | Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant | B | 8.66 | pKi | 2.2 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| 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 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 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 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]
