L745870 [Ligand Id: 3303] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL267014 (L-745870) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Inhibition of alpha1C adrenergic receptor (unknown origin) | B | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Inhibition of alpha1B adrenergic receptor (unknown origin) | B | 5.54 | pKi | 2900 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | Inhibition of alpha2A adrenergic receptor (unknown origin) | B | 6.77 | pKi | 170 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | Inhibition of alpha2B adrenergic receptor (unknown origin) | B | 6.8 | pKi | 160 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Inhibition of alpha2C adrenergic receptor (unknown origin) | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Binding affinity to cloned Opioid receptor delta 1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 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 | pKi | >10000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136] | ||||||||
| ChEMBL | Binding affinity was evaluated for the displacement of [3H]-SCH- 23390 against bovine Dopamine receptor D1 | B | 5 | pKi | 9900 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464] |
| ChEMBL | In vitro binding affinity at human cloned dopamine receptor D1 stably expressed in CHO cells by [3H]-SCH- 23390 displacement. | B | 5 | pKi | 9900 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
| ChEMBL | Displacement of [3H]SCH23390 from bovine dopamine D1 receptor | B | 5 | pKi | 9900 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | In vitro binding affinity to cloned rat Dopamine receptor D1 measured by displacement of radioligand [3H]SCH-23,982 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | In vitro binding affinity at human cloned dopamine receptor D2 (long) stably expressed in CHO cells by [3H]-Spiperone displacement. | B | 4.27 | pKi | 54000 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
| ChEMBL | Displacement of [3H]SCH23390 from human cloned dopamine D2 long receptor expressed in CHO cells | B | 4.27 | pKi | 54000 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
| ChEMBL | Binding affinity to dopamine D2 | B | 4.27 | pKi | 53703.18 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
| ChEMBL | Displacement of [3H] Spiperone from human D2L receptor expressed in CHO cells by competitive radioligand binding assay | B | 4.33 | pKi | 47000 | nM | Ki | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | In vitro binding affinity at human cloned dopamine receptor D2 (short) stably expressed in CHO cells by [3H]spiperone displacement. | B | 4.42 | pKi | 38000 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
| ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D2 short receptor expressed in CHO cells | B | 4.42 | pKi | 38000 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
| ChEMBL | Displacement of [3H] Spiperone from human D2S receptor expressed in CHO cells by competitive radioligand binding assay | B | 4.48 | pKi | 33000 | nM | Ki | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method | B | 5.79 | pKi | 1621.81 | nM | Ki | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| ChEMBL | Binding affinity to D2R (unknown origin) assessed as inhibition constant | B | 6.02 | pKi | 960 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| ChEMBL | Binding affinity towards cloned human Dopamine receptor D2 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 6.02 | pKi | 960 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
| ChEMBL | Ability to displace [3H]spiperone from cloned human dopamine D2 receptor stably expressed in CHO cells | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 585-588 [PMID:10098669] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by liquid scintillation counting | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor by PDSP assay | B | 6.02 | pKi | 960 | nM | Ki | Bioorg Med Chem (2014) 22: 3105-3114 [PMID:24800940] |
| ChEMBL | Inhibition of human dopamine D2 receptor | B | 6.02 | pKi | 960 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | In vitro binding affinity was measured at the cloned human Dopamine receptor D2 using [3H]spiroperidol as radioligand. | B | 6.04 | pKi | 920 | nM | Ki | J Med Chem (1998) 41: 4903-4909 [PMID:9822559] |
| ChEMBL | Binding affinity at Dopamine receptor D2 in CHO cells by radioligand displacement. | B | 6.04 | pKi | 908 | nM | Ki | J Med Chem (1999) 42: 5181-5187 [PMID:10602703] |
| ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D2 expressed in CHO cells | B | 6.04 | pKi | 908 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1499-1502 [PMID:9873377] |
| ChEMBL | Binding affinity against human Dopamine receptor D2 using [3H]spiperone as radioligand | B | 6.35 | pKi | 448 | nM | Ki | J Med Chem (2004) 47: 2348-2355 [PMID:15084133] |
| Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
| ChEMBL | Binding affinity was evaluated for the displacement of [3H]spiperone against bovine Dopamine receptor D2 | B | 5.21 | pKi | 6100 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro binding affinity to rat Dopamine receptor D2 measured by displacement of the radioligand [3H]spiperone | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 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 | 4.19 | pKi | 65000 | nM | Ki | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D3 expressed in CHO cell membrane | B | 4.51 | pKi | 30902.95 | nM | Ki | J Med Chem (2007) 50: 489-500 [PMID:17266201] |
| ChEMBL | Binding affinity evaluated for the displacement of [3H]-spiperone against human dopamine receptor D3 | B | 4.54 | pKi | 29000 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464] |
| ChEMBL | In vitro binding affinity at human cloned dopamine receptor D3 stably expressed in CHO cells by [3H]spiperone displacement. | B | 4.66 | pKi | 22000 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
| ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor expressed in CHO cells | B | 4.66 | pKi | 22000 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
| ChEMBL | Displacement of [3H]spiperone from human Dopamine receptor D3 expressed in CHO cells | B | 5.52 | pKi | >3030 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1499-1502 [PMID:9873377] |
| ChEMBL | Binding affinity at Dopamine receptor D3 in CHO cells by radioligand displacement. | B | 5.52 | pKi | >3030 | nM | Ki | J Med Chem (1999) 42: 5181-5187 [PMID:10602703] |
| ChEMBL | Inhibition of human dopamine D3 receptor | B | 5.64 | pKi | 2310 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | Binding affinity to D3R (unknown origin) assessed as inhibition constant | B | 5.64 | pKi | 2310 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| ChEMBL | Ability to displace [3H]-spiperone from cloned human dopamine D3 receptor stably expressed in CHO cells | B | 5.64 | pKi | 2300 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 585-588 [PMID:10098669] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor by PDSP assay | B | 5.64 | pKi | 2300 | nM | Ki | Bioorg Med Chem (2014) 22: 3105-3114 [PMID:24800940] |
| ChEMBL | Binding affinity towards cloned human Dopamine receptor D3 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 5.64 | pKi | 2300 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human D3R receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method | B | 6.42 | pKi | 380.19 | nM | Ki | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| ChEMBL | In vitro binding affinity to cloned rat Dopamine receptor D3 measured by displacement of the radioligand [3H]sulpiride | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method | B | 8.65 | pKi | 2.24 | nM | Ki | J Med Chem (2018) 61: 3712-3725 [PMID:29589445] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human D4.4 receptor expressed in HEK293T cell membrane incubated for 1 hr by MicroBeta scintillation counting method | B | 8.65 | pKi | 2.24 | nM | Ki | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| ChEMBL | Binding affinity at Dopamine receptor D4 in CHO cells by radioligand displacement. | B | 9.04 | pKi | 0.91 | nM | Ki | J Med Chem (1999) 42: 5181-5187 [PMID:10602703] |
| ChEMBL | In vitro binding affinity at human dopamine D4 receptor expressed in CHO cells by [3H]spiperone displacement. | B | 9.04 | pKi | 0.91 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 1499-1502 [PMID:9873377] |
| ChEMBL | Displacement of [3H] Spiperone from human D4.4 receptor expressed in CHO cells by competitive radioligand binding assay | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D4.4 receptor expressed in CHO cells | B | 9.21 | pKi | 0.62 | nM | Ki | Bioorg Med Chem (2009) 17: 4448-4458 [PMID:19481941] |
| ChEMBL | In vitro binding affinity at human cloned dopamine receptor D4 stably expressed in CHO cells by [3H]spiperone displacement. | B | 9.21 | pKi | 0.62 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 expressed in CHO cell membrane | B | 9.21 | pKi | 0.62 | 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 | 9.21 | pKi | 9.21 | D4 | Log Ki | J Med Chem (2001) 44: 1151-1157 [PMID:11312915] |
| ChEMBL | Binding affinity evaluated for the displacement of [3H]spiperone against human dopamine receptor D4 | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 97-102 [PMID:9990464] |
| ChEMBL | Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane | B | 9.22 | pKi | 0.6 | nM | Ki | Eur J Med Chem (2022) 244: 114840-114840 [PMID:36283180] |
| ChEMBL | Displacement of [3H]N-methylspiperone from D4 receptor in HEK293 cell membrane | B | 9.26 | pKi | 0.55 | nM | Ki | Eur J Med Chem (2022) 244: 114840-114840 [PMID:36283180] |
| ChEMBL | Ability to displace [3H]spiperone from cloned human dopamine D4 receptor stably expressed in HEK293 cells | B | 9.37 | pKi | 0.43 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 585-588 [PMID:10098669] |
| ChEMBL | Binding affinity towards cloned human Dopamine receptor D4 stably expressed in CHO cells was evaluated using [3H]spiperone as radioligand | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (1996) 39: 1941-1942 [PMID:8642550] |
| ChEMBL | Inhibition of human dopamine D4 receptor | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | In vitro binding affinity to human Dopamine receptor D4 | B | 9.37 | pKi | 0.43 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| ChEMBL | Binding affinity towards human dopamine receptor D4 | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
| ChEMBL | Displacement of [125I]DOI from human dopamine D4 receptor by liquid scintillation counting | B | 9.37 | pKi | 0.43 | nM | Ki | Bioorg Med Chem (2009) 17: 1716-1723 [PMID:19155177] |
| ChEMBL | Displacement of [3H]-spiperone from human D4 receptor expressed in HEK293 cells assessed as inhibition constant | B | 9.37 | pKi | 0.43 | nM | Ki | Eur J Med Chem (2021) 212: 113141-113141 [PMID:33422983] |
| ChEMBL | In vitro binding affinity was measured at the cloned human Dopamine receptor D4.2 using [3H]YM-09151-2 as radioligand. | B | 9.37 | pKi | 0.43 | nM | Ki | J Med Chem (1998) 41: 4903-4909 [PMID:9822559] |
| ChEMBL | Binding affinity against human Dopamine receptor D4 by [3H]-spiperone displacement. | B | 9.4 | pKi | 0.4 | nM | Ki | J Med Chem (2004) 47: 2348-2355 [PMID:15084133] |
| GtoPdb | - | - | 9.41 | pKi | 0.39 | nM | Ki | J Med Chem (1996) 39: 1941-2 [PMID:8642550] |
| ChEMBL | Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced Gi protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay | F | 5.71 | pIC50 | 1949.84 | nM | IC50 | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| ChEMBL | Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced beta arrestin-2 recruitment pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay | F | 6.79 | pIC50 | 162.18 | nM | IC50 | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| ChEMBL | Antagonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as inhibition of dopamine-induced G0 protein activation pretreated for 10 mins followed by dopamine addition and measured after 2.5 mins by BRET assay | F | 6.84 | pIC50 | 144.54 | nM | IC50 | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| ChEMBL | Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced RLuc8-fused Galphai1 activation preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay | B | 7.03 | pIC50 | 93.33 | nM | IC50 | J Med Chem (2018) 61: 3712-3725 [PMID:29589445] |
| ChEMBL | Antagonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as inhibition of dopamine-induced mVenus-fused beta-arrestin2 recruitment preincubated for 15 mins followed by dopamine induction measured after 2 mins by BRET assay | B | 7.37 | pIC50 | 42.66 | nM | IC50 | J Med Chem (2018) 61: 3712-3725 [PMID:29589445] |
| ChEMBL | Effective concentration against human Dopamine receptor D4 | B | 5.65 | pEC50 | 2230 | nM | EC50 | J Med Chem (2004) 47: 2348-2355 [PMID:15084133] |
| ChEMBL | Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay | F | 7.57 | pEC50 | 27 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
| D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| ChEMBL | In vitro binding affinity to rat Dopamine receptor D4 measured by displacement of the radioligand [3H]spiperone | B | 8.43 | pKi | 3.7 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| ChEMBL | Displacement of [3H]N-methylspiperone from rat dopamine D4 receptor by PDSP assay | B | 9.37 | pKi | 0.43 | nM | Ki | Bioorg Med Chem (2014) 22: 3105-3114 [PMID:24800940] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Inhibition of human dopamine D5 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| D5 receptor/Dopamine D5 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2281] [GtoPdb: 218] [UniProtKB: P25115] | ||||||||
| ChEMBL | In vitro binding affinity to cloned rat D5 receptor measured by displacement of radioligand [3H]SCH-23,982 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| GluN2D/GluN3B/GluN1/GluN2A/GluN2B/GluN2C/GluN3A/Glutamate [NMDA] receptor in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2094124] [GtoPdb: 459, 461, 455, 456, 457, 458, 460] [UniProtKB: O15399, O60391, Q05586, Q12879, Q13224, Q14957, Q8TCU5] | ||||||||
| ChEMBL | Binding affinity for N-methyl-D-aspartate glutamate receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| GluN1/GluN2A/GluN2B/GluN2C/GluN2D/GluN3B/GluN3A/Glutamate NMDA receptor in Rat (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL1907608] [GtoPdb: 455, 456, 457, 458, 459, 461, 460] [UniProtKB: P35439, Q00959, Q00960, Q00961, Q62645, Q8VHN2, Q9R1M7] | ||||||||
| ChEMBL | Binding affinity to PCP site of rat N-methyl-D-aspartate glutamate receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Binding affinity to cloned Histamine H1 receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Binding affinity to cloned Opioid receptor kappa 1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Binding affinity to cloned Opioid receptor mu 1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Binding affinity to cloned Muscarinic acetylcholine receptor M1 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| ChEMBL | Binding affinity to cloned Muscarinic acetylcholine receptor M2 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Binding affinity to cloned Muscarinic acetylcholine receptor M3 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Binding affinity to cloned Muscarinic acetylcholine receptor M4 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Binding affinity to cloned Muscarinic acetylcholine receptor M5 | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Inhibition of serotonin 5-HT1A receptor (unknown origin) | B | 5.11 | pKi | 7800 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| ChEMBL | In vitro binding affinity to human 5-hydroxytryptamine 1A receptor | B | 5.18 | pKi | 6620.9 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Binding affinity to cloned human 5-hydroxytryptamine 1B receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | In vitro binding affinity to human 5-hydroxytryptamine 1D receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Binding affinity to cloned human 5-hydroxytryptamine 1E receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity to cloned human 5-hydroxytryptamine 2A receptor | B | 6.34 | pKi | 453 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| ChEMBL | Inhibition of serotonin 5-HT2 receptor (unknown origin) | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2017) 60: 7233-7243 [PMID:28489950] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity to cloned human 5-hydroxytryptamine 2C receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity to cloned human 5-hydroxytryptamine 5A receptor | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | In vitro binding affinity to human 5-hydroxytryptamine 6 receptor | B | 5.78 | pKi | 1656.2 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | In vitro binding affinity to human 5-hydroxytryptamine 7 receptor | B | 6.65 | pKi | 226.3 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1375-1377 [PMID:11378358] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | Binding affinity towards sigma receptor was determined | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2001) 44: 477-501 [PMID:11170639] |
| ChEMBL | Displacement of [3H] Pentazocine from sigma 1 receptor in HEK293 cell membrane | B | 7 | pKi | 101 | nM | Ki | Eur J Med Chem (2022) 244: 114840-114840 [PMID:36283180] |
| ChEMBL | Displacement of [3H] Pentazocine from sigma 1 receptor in HEK293 cell membrane | B | 7 | pKi | 100 | nM | Ki | Eur J Med Chem (2022) 244: 114840-114840 [PMID:36283180] |
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]
