[3H]SB269970 [Ligand Id: 3247] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL282199 (SB-269970) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| ChEMBL | Binding affinity towards Alpha-1B adrenergic receptor | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity towards Dopamine receptor D2 (human cloned receptor) in CHO cells using [125I]iodosulpiride radioligand. | B | 6.5 | pKi | 316.23 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| ChEMBL | Displacement of [3H]raclopride from human dopamine receptor D2A expressed in mouse Ltk cells | B | 6.5 | pKi | 316 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Binding affinity towards Dopamine receptor D3 (human cloned receptor) in CHO cells using [125I]iodosulpiride radioligand. | B | 5.6 | pKi | 2511.89 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor (human cloned receptor) in HEK293 cells using [3H]8-OH-DPAT as radioligand; | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-hydroxytryptamine 1A receptor expressed in CHO cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
| ChEMBL | Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2014) 85: 716-726 [PMID:25128671] |
| ChEMBL | Antagonist activity at 5-HT1A receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| ChEMBL | Binding affinity to 5HT1A receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from recombinant human 5-HT1A receptor expressed in CHOK1 cell membranes after 1 hr by liquid scintillation counting method | B | 5.04 | pKi | 9024 | nM | Ki | Bioorg Med Chem (2017) 25: 1250-1259 [PMID:28063784] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | B | 5.04 | pKi | 9024 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505] |
| ChEMBL | Displacement of [3H]-5-HT from human 5-HT1A receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis | B | 5.04 | pKi | 9024 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells after 1 hr | B | 5.3 | pKi | >5000 | nM | Ki | Eur J Med Chem (2012) 56: 348-360 [PMID:22926225] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT1A receptor expressed in HEK293 cells | B | 8.3 | pKi | <5 | nM | Ki | Bioorg Med Chem (2016) 24: 5730-5740 [PMID:27717652] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor in rat hippocampus | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4827-4831 [PMID:19560916] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Binding affinity to 5HT1B receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Binding affinity to 5HT1D receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 1D receptor in CHO cells using [3H]5-HT as radioligand. | B | 5.8 | pKi | 1584.89 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Binding affinity to 5HT1E receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 1E receptor in CHO cells using [3H]5-HT as radioligand. | B | 5.2 | pKi | <6309.57 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1F receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand. | B | 5.5 | pKi | <3162.28 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 2A receptor (human cloned receptor) in HEK 293 cells using [3H]ketanserin as radioligand. | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| ChEMBL | Binding affinity to 5HT2A receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Displacement of [3H]-ketanserin from human 5-HT2A receptor expressed in HEK293 cells | B | 8.3 | pKi | <5 | nM | Ki | Bioorg Med Chem (2016) 24: 5730-5740 [PMID:27717652] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Binding affinity to 5HT2A receptor in rat cortex | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4827-4831 [PMID:19560916] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand | B | 5 | pKi | 10000 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| ChEMBL | Binding affinity to 5HT2B receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 2C receptor in HEK293 cells, using [3H]mesulergine as radioligand | B | 5 | pKi | <10000 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| ChEMBL | Binding affinity to 5HT2C receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Binding affinity to 5HT3 receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Binding affinity to 5HT4 receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 4 receptor | B | 5.9 | pKi | 1258.93 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| 5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 5 receptor | B | 7.19 | pKi | 65 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 5A receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand. | B | 7.2 | pKi | 63.1 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| ChEMBL | Binding affinity to 5HT5A receptor (unknown origin) | B | 9.11 | pKi | 0.78 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity to 5HT6 receptor (unknown origin) | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 6 receptor (human cloned receptor) in HEK 293 cells using [3H]mesulergine as radioligand. | B | 5.2 | pKi | 6309.57 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Binding affinity to 5HT7 receptor | B | 8.01 | pKd | 9.7 | nM | Kd | Eur J Med Chem (2011) 46: 3455-3461 [PMID:21620533] |
| GtoPdb | - | - | 8.92 | pKd | 1.2 | nM | Kd | Br J Pharmacol (2000) 130: 409-17 [PMID:10807680] |
| ChEMBL | Displacement of [3H]-5-HT from human 5HT7 receptor expressed in CHO-K1 cells incubated for 40 mins in presence of serotonin by liquid scintillation counter | B | 8.72 | pKi | 1.9 | nM | Ki | Eur J Med Chem (2019) 183: 111690-111690 [PMID:31526973] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 7 receptor | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (2003) 46: 2795-2812 [PMID:12825922] |
| ChEMBL | Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem (2016) 24: 5730-5740 [PMID:27717652] |
| ChEMBL | Binding affinity to 5HT7 receptor (unknown origin) | B | 8.9 | pKi | 1.26 | nM | Ki | Bioorg Med Chem (2013) 21: 2568-2576 [PMID:23541835] |
| ChEMBL | Binding affinity to human 5-HT7 receptor by radioligand binding assay | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2018) 61: 8475-8503 [PMID:29767995] |
| ChEMBL | Displacement of [3H]5-HT from human 5HT7 receptor transfected in CFO-K1 cells after 30 mins by liquid scintillation spectrometry | B | 8.9 | pKi | 1.26 | nM | Ki | Eur J Med Chem (2014) 85: 716-726 [PMID:25128671] |
| ChEMBL | Displacement of [3H]-5-CT from human 5-HT7a receptor expressed in HEK293 cells | B | 8.9 | pKi | 1.26 | nM | Ki | Bioorg Med Chem (2016) 24: 5730-5740 [PMID:27717652] |
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 7 receptor (a) (human cloned receptor) in HEK 293 cells using [3H]5-CT as radioligand. | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2000) 43: 342-345 [PMID:10669560] |
| ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 7 receptor was determined in HEK293 cells using [3H]5-CT as radioligand | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
| ChEMBL | Antagonist activity at 5-HT7 receptor (unknown origin) | B | 8.9 | pKi | 1.25 | nM | Ki | Eur J Med Chem (2019) 183: 111705-111705 [PMID:31581003] |
| ChEMBL | Displacement of [3H]-5-CT from human 5-HT7 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem (2011) 19: 6750-6759 [PMID:22001327] |
| ChEMBL | Binding affinity to human cloned 5HT7 receptor expressed in HEK293 cells | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 4827-4831 [PMID:19560916] |
| ChEMBL | Displacement of [3H]-5-CT from human 5-HT7b receptor expressed in HEK293 cells after 1 hr | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2012) 56: 348-360 [PMID:22926225] |
| ChEMBL | Binding affinity to 5HT7 receptor | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 42-44 [PMID:21159507] |
| ChEMBL | Binding affinity towards human 5-hydroxytryptamine 7 receptor on HEK293 cells using radioligand [3H]LSD | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2451-2454 [PMID:12161155] |
| ChEMBL | Displacement of [3H]-8-OH-DPAT from human 5-HT7 receptor expressed in CHOK1 cells after 30 mins by liquid scintillation counting analysis | B | 9.15 | pKi | 0.71 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 1427-1430 [PMID:25759032] |
| ChEMBL | Displacement of [3H]-5-HT from human 5-HT7 receptor expressed in CHOK1 cell membranes after 30 mins by liquid scintillation spectrometry | B | 9.15 | pKi | 0.71 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4052-4056 [PMID:27396505] |
| ChEMBL | Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method | B | 9.15 | pKi | 0.71 | nM | Ki | Bioorg Med Chem (2017) 25: 1250-1259 [PMID:28063784] |
| ChEMBL | Displacement of [3H]D-lysergic acid diethylamide from 5HT7R (unknown origin) expressed in HEK293 cell membranes incubated for 1.5 hrs in absence of light by liquid scintillation counting | B | 9.47 | pKi | 0.34 | nM | Ki | Eur J Med Chem (2016) 123: 180-190 [PMID:27475109] |
| ChEMBL | Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method | B | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (2018) 61: 7218-7233 [PMID:30028132] |
| ChEMBL | Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method | B | 9.47 | pKi | 0.34 | nM | Ki | Eur J Med Chem (2016) 110: 302-310 [PMID:26852005] |
| ChEMBL | Displacement of [3H]LSD from 5-HT7R (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem (2014) 22: 4587-4596 [PMID:25127461] |
| ChEMBL | Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting | B | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Displacement of [3H]-LSD from 5HT7 receptor (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by liquid scintillation counting | B | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Displacement of [3H]LSD from 5-HT7 receptor (unknown origin) expressed in CHO-K1 cells by liquid scintillation counting method | B | 9.47 | pKi | 0.34 | nM | Ki | Eur J Med Chem (2016) 110: 302-310 [PMID:26852005] |
| ChEMBL | Displacement of [3H]LSD from human 5-HT7 receptor expressed in HEK cell membranes after 1.5 hrs by microbeta scintillation counting method | B | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (2018) 61: 7218-7233 [PMID:30028132] |
| ChEMBL | Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay | F | 8.43 | pIC50 | 3.71 | nM | IC50 | Eur J Med Chem (2016) 123: 180-190 [PMID:27475109] |
| ChEMBL | Antagonist activity at human 5-HT7R expressed in HEK293 cells assessed as inhibition of serotonin stimulated-cAMP levels preincubated for 10 mins followed by serotonin stimulation after 30 mins by D2-dye based fluorescence assay | F | 8.43 | pIC50 | 3.71 | nM | IC50 | Eur J Med Chem (2016) 123: 180-190 [PMID:27475109] |
| ChEMBL | Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay | B | 8.58 | pIC50 | 2.63 | nM | IC50 | Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628] |
| ChEMBL | Antagonist activity at human recombinant 5-HT7 receptor expressed in CHOK1 cells measured after 60 mins in the presence of serotonin by LANCE TR-FRET assay | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem (2019) 27: 4163-4173 [PMID:31383628] |
| ChEMBL | Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay | F | 9.03 | pIC50 | 0.93 | nM | IC50 | J Med Chem (2018) 61: 7218-7233 [PMID:30028132] |
| ChEMBL | Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis | F | 9.03 | pIC50 | 0.93 | nM | IC50 | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| ChEMBL | Antagonist activity at human 5-HT7 receptor expressed in CHO-K1 cells assessed as decrease in serotonin-induced cAMP level after 1 hr by TR-FRET assay | F | 9.03 | pIC50 | 0.93 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2039-2049 [PMID:29730027] |
| ChEMBL | Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as inhibition of Gs protein-mediated cAMP accumulation by luminescence-based assay | F | 9.05 | pIC50 | 0.9 | nM | IC50 | J Med Chem (2018) 61: 7218-7233 [PMID:30028132] |
| ChEMBL | Antagonist activity at human 5-HT7 receptor expressed in HEK293 cells assessed as reduction in cAMP accumulation incubated for 30 mins by microplate reader analysis | F | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2021) 64: 13766-13779 [PMID:34519505] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine receptor 7 on rat hypothalamus membranes using [3H]5-CT as radioligand. | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (2003) 46: 5638-5650 [PMID:14667218] |
| ChEMBL | Displacement of [3H]5-HT from rat 5-hydroxytryptamine 7 receptor expressed in CHO cells | B | 8.9 | pKi | 1.26 | nM | Ki | J Med Chem (2001) 44: 1337-1340 [PMID:11311055] |
| ChEMBL | Binding affinity towards rat 5-HT7 receptor expressed in HEK cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2004) 47: 5451-5466 [PMID:15481983] |
| Serotonin 7 (5-HT7) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5494] [UniProtKB: P50407] | ||||||||
| ChEMBL | Antagonist activity at 5HT7 receptor assessed as inhibition of 5-carboxamidotryptamine mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction | F | 7.48 | pKd | 33.11 | nM | Kd | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| ChEMBL | Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 3-(2-aminoethyl)-1H-indole-5-carboxamide mediated relaxation of substance P-induced contraction | F | 7.48 | pKd | 33.11 | nM | Kd | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Antagonist activity at 5HT7 receptor assessed as inhibition of N-(4-Cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction | F | 7.69 | pKd | 20.42 | nM | Kd | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| ChEMBL | Antagonist activity at 5HT7 receptor assessed as inhibition of 2-[6-[4-(2-Diphenyl)-1-piperazinyl]-1-oxohexyl]-1,2,3,4-tetrahydroisoquinoline mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction | F | 7.8 | pKd | 15.85 | nM | Kd | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| ChEMBL | Antagonist activity at 5HT7 receptor assessed as inhibition of 6-(4-Biphenyl-2-yl-piperazin-1-yl)-hexanoic acid (1,2,3,4-tetrahydro-naphthalen-1-yl)-amide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction | F | 7.84 | pKd | 14.45 | nM | Kd | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| ChEMBL | Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-diphenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction | F | 7.84 | pKd | 14.45 | nM | Kd | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-(2-dimethylaminophenyl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction | F | 7.9 | pKd | 12.59 | nM | Kd | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Antagonist activity at 5HT7 receptor assessed as inhibition of 4-(2-Diphenyl)-N-(4-pyridinylmethyl)-1-piperazinehexanamide mediated relaxation of substance P-induced Dunkin-Hartley guinea pig ileum contraction | F | 7.96 | pKd | 10.96 | nM | Kd | J Med Chem (2008) 51: 5813-5822 [PMID:18800769] |
| ChEMBL | Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 4-[2-(1-methylethyl)phenyl]-N-(1,2,3,4-tetrahydronaphthalen-1-yl)-1-piperazine hexanamide mediated relaxation of substance P-induced contraction | F | 8.05 | pKd | 8.91 | nM | Kd | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-phenylpiperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction | F | 8.1 | pKd | 7.94 | nM | Kd | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-nitrophenyl)piperazin-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction | F | 8.2 | pKd | 6.31 | nM | Kd | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
| ChEMBL | Antagonist activity at 5HT7 receptor in guinea pig ileum assessed as effect on 6-(4-(2-chlorophenyl)piperazine-1-yl)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)hexanamide mediated relaxation of substance P-induced contraction | F | 8.4 | pKd | 3.98 | nM | Kd | J Med Chem (2007) 50: 4214-4221 [PMID:17649988] |
ChEMBL data shown on this page come from version 32:
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]
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