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ChEMBL ligand: CHEMBL444309 (L-741742) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Binding affinity to D2R (unknown origin) assessed as inhibition constant | B | 4.77 | pKi | >17000 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
ChEMBL | Affinity to displace [3H]spiperone from cloned human Dopamine receptor D2 stably expressed in CHO cell lines | B | 5.77 | pKi | >1700 | nM | Ki | J Med Chem (1999) 42: 2706-2715 [PMID:10411491] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells | B | 5.77 | pKi | >1700 | nM | Ki | J Med Chem (1996) 39: 1943-1945 [PMID:8642551] |
ChEMBL | Ability to displace [3H]spiperone from human dopamine receptor D2 stably expressed in CHO cells. | B | 5.77 | pKi | >1700 | nM | Ki | J Med Chem (1997) 40: 2374-2385 [PMID:9240352] |
ChEMBL | Inhibition of human dopamine D2 receptor | B | 5.77 | pKi | >1700 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
ChEMBL | Affinity to displace [3H]spiperone from cloned human Dopamine receptor D3 (hD3) stably expressed in HEK393 cell lines | B | 6.11 | pKi | 770 | nM | Ki | J Med Chem (1999) 42: 2706-2715 [PMID:10411491] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells | B | 6.11 | pKi | 770 | nM | Ki | J Med Chem (1996) 39: 1943-1945 [PMID:8642551] |
ChEMBL | Ability to displace [3H]spiperone from human dopamine receptor D3 (hD3) receptor stably expressed in HEK293 cells. | B | 6.11 | pKi | 770 | nM | Ki | J Med Chem (1997) 40: 2374-2385 [PMID:9240352] |
ChEMBL | Binding affinity to D3R (unknown origin) assessed as inhibition constant | B | 6.11 | pKi | 770 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
ChEMBL | Inhibition of human dopamine D3 receptor | B | 6.32 | pKi | 480 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
ChEMBL | Affinity to displace [3H]spiperone from cloned human Dopamine receptor D4 stably expressed in HEK393 cell lines | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1999) 42: 2706-2715 [PMID:10411491] |
ChEMBL | Binding affinity towards human dopamine receptor D4 | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D4 expressed in HEK293 cells | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1996) 39: 1943-1945 [PMID:8642551] |
ChEMBL | Ability to displace [3H]spiperone from human dopamine receptor D4 (hD4) receptor stably expressed in HEK293 cells. | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (1997) 40: 2374-2385 [PMID:9240352] |
ChEMBL | Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant | B | 8.46 | pKi | 3.5 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
GtoPdb | - | - | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (1996) 39: 1943-5 [PMID:8642551] |
ChEMBL | Inhibition of human dopamine D4 receptor | B | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
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]