ChEMBL ligand: CHEMBL230963
D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] There should be some charts here, you may need to enable JavaScript!
FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] There should be some charts here, you may need to enable JavaScript!
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] 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
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Displacement of [3H]-methylspiperone from recombinant human D2 receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method	B	6	pKi	>1000	nM	Ki	J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL	GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4	F	5	pIC50	>10000	nM	IC50	EUbOPEN Chemogenomics Library - GPCR Dose-Respose
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb	-	-	8.6	pKi	-	-	-	Br J Pharmacol (2009) 156: 338-53 [PMID:19154445]
ChEMBL	Displacement of [3H]8-OH-DPAT from human 5-HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by Microbeta2 scintillation counting method	B	8.66	pKi	2.19	nM	Ki	J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
ChEMBL	Displacement of [3H]8-OH-DPAT from recombinant human 5HT1A receptor stably expressed in CHO-K1 cell membranes measured after 60 mins by microbeta2 scintillation counting method	B	8.66	pKi	2.19	nM	Ki	J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL	Agonist activity at human 5HT1A receptor expressed in C6 cells assessed as stimulation of [35S]GTPgammaS binding	F	6.41	pEC50	389.05	nM	EC50	J Med Chem (2007) 50: 5024-5033 [PMID:17803293]
ChEMBL	Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay	F	6.52	pEC50	302	nM	EC50	J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
ChEMBL	Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in calcium mobilization measured at 2 sec intervals for 180 secs by Fluo-4AM dye based fluorescence assay	F	6.61	pEC50	245.47	nM	EC50	J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL	Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as stimulation of beta-arrestin recruitment measured after 5 hrs by Tango assay	B	6.71	pEC50	194.98	nM	EC50	J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL	Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay	B	6.71	pEC50	194.98	nM	EC50	J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
ChEMBL	Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay	F	7.22	pEC50	60.26	nM	EC50	J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
ChEMBL	Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 40 mins by LANCE Ultra cAMP kit-based TR-FRET assay	F	7.22	pEC50	60.26	nM	EC50	J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL	Biased agonist activity at human recombinant 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation levels incubated for 15 mins by Alphalisa assay	B	8.33	pEC50	4.68	nM	EC50	J Med Chem (2019) 62: 2750-2771 [PMID:30721053]
ChEMBL	Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay	B	8.33	pEC50	4.68	nM	EC50	J Med Chem (2020) 63: 10946-10971 [PMID:32883072]
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 cortex membrane	B	8.65	pKi	2.24	nM	Ki	J Med Chem (2007) 50: 5024-5033 [PMID:17803293]

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]