ChEMBL ligand: CHEMBL389348 (SB-290157)
C3a receptor/C3a anaphylatoxin chemotactic receptor in Human [ChEMBL: CHEMBL4761] [GtoPdb: 31] [UniProtKB: Q16581] 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
C3a receptor/C3a anaphylatoxin chemotactic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4761] [GtoPdb: 31] [UniProtKB: Q16581]
ChEMBL	Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	F	5.4	pIC50	3981.07	nM	IC50	J Med Chem (2020) 63: 529-541 [PMID:31910011]
ChEMBL	Antagonist activity at human C3a receptor in human U937 cells assessed as inhibition of intracellular calcium mobilization	F	5.89	pIC50	1300	nM	IC50	J Med Chem (2010) 53: 4938-4948 [PMID:20527893]
ChEMBL	Antagonist activity at C3a receptor in human MDM cells assessed as inhibition of C3a-induced intracellular calcium release preincubated for 30 mins followed by C3a addition and measured at 1 sec interval for => 200 secs by Fluo-3 AM dye-based FLIPR assay	F	5.89	pIC50	1300	nM	IC50	J Med Chem (2020) 63: 529-541 [PMID:31910011]
ChEMBL	Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay	F	5.9	pIC50	1258.93	nM	IC50	J Med Chem (2014) 57: 8459-8470 [PMID:25259874]
ChEMBL	Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition	B	6.27	pIC50	540	nM	IC50	J Med Chem (2020) 63: 529-541 [PMID:31910011]
ChEMBL	Inhibition of human C3a receptor expressed on HMC1 cells by SPA assay	B	6.3	pIC50	501.19	nM	IC50	Bioorg Med Chem Lett (2007) 17: 3258-3261 [PMID:17467987]
ChEMBL	Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition	B	6.3	pIC50	501.19	nM	IC50	J Med Chem (2020) 63: 529-541 [PMID:31910011]
ChEMBL	Displacement of 125I-C3a from human C3aR expressed in RBL-2H3 cells	B	6.7	pIC50	200	nM	IC50	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
ChEMBL	Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting	B	6.85	pIC50	140	nM	IC50	J Med Chem (2010) 53: 4938-4948 [PMID:20527893]
ChEMBL	Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting	B	6.9	pIC50	125.89	nM	IC50	J Med Chem (2010) 53: 4938-4948 [PMID:20527893]
ChEMBL	Antagonist activity at human C3aR expressed in RBL-2H3 cells assessed as inhibition of C3a-induced intracellular calcium mobilization	F	7.55	pIC50	28	nM	IC50	J Med Chem (2018) 61: 3253-3276 [PMID:28977749]
GtoPdb	-	-	7.6	pIC50	28	nM	IC50	J Immunol (2001) 166: 6341-8 [PMID:11342658]; Front Pharmacol (2020) 11: 591398 [PMID:33551801]
ChEMBL	Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method	B	8	pIC50	10	nM	IC50	J Med Chem (2014) 57: 8459-8470 [PMID:25259874]
ChEMBL	Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method	B	8	pIC50	10	nM	IC50	J Med Chem (2014) 57: 8459-8470 [PMID:25259874]
ChEMBL	Antagonist activity against C3AR in HMDMs assessed as inhibition of C3a-induced intracellular calcium release by Fluo-3 AM dye based FLIPR assay	F	8.89	pIC50	1.3	nM	IC50	J Med Chem (2014) 57: 8459-8470 [PMID:25259874]

ChEMBL data shown on this page come from version 33:

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]