SB269970 [Ligand Id: 3233] 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] |
| 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] |
| GtoPdb | - | - | 8.9 | pKi | - | - | - | Br J Pharmacol (2000) 130: 409-17 [PMID:10807680] |
| 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 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]
