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 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]