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Assay Detail

CHEMBL889062

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human C3a receptor expressed on HMC1 cells by SPA assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HMC1
Confidence 9 — Direct single protein target
Curated By Expert

Target

C3a anaphylatoxin chemotactic receptor (CHEMBL4761)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of new C3aR ligands. Part 1: arginine derivatives.
Denonne F, Binet S, Burton M, Collart P, Dipesa A, Ganguly T, Giannaras A, Kumar S, Lewis T, Maounis F, Nicolas JM, Mansley T, Pasau P, Preda D, Stebbins K, Volosov A, Zou D.
Bioorg Med Chem Lett (2007) 17 : 3258 -3261
PubMed 17467987 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.29 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387755 1 7.80
CHEMBL229005 1 7.50
CHEMBL230034 1 7.20
CHEMBL231405 1 7.10
CHEMBL231303 1 6.90
CHEMBL229006 1 6.80
CHEMBL427268 1 6.70
CHEMBL231404 1 6.70
CHEMBL265866 1 6.70
CHEMBL228634 1 6.50
CHEMBL394538 1 6.50
CHEMBL389349 1 6.50
CHEMBL389348 1 6.30
CHEMBL228582 1 6.10
CHEMBL394539 1 6.10
CHEMBL228847 1 6.10
CHEMBL228901 1 6.10
CHEMBL387686 1 5.80
CHEMBL228635 1 5.40
CHEMBL390834 1 5.20
CHEMBL228900 1 4.30
CHEMBL228846 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387755 IC50 = 15.85 nM 7.80
CHEMBL229005 IC50 = 31.62 nM 7.50
CHEMBL230034 IC50 = 63.1 nM 7.20
CHEMBL231405 IC50 = 79.43 nM 7.10
CHEMBL231303 IC50 = 125.89 nM 6.90
CHEMBL229006 IC50 = 158.49 nM 6.80
CHEMBL427268 IC50 = 199.53 nM 6.70
CHEMBL231404 IC50 = 199.53 nM 6.70
CHEMBL265866 IC50 = 199.53 nM 6.70
CHEMBL228634 IC50 = 316.23 nM 6.50
CHEMBL394538 IC50 = 316.23 nM 6.50
CHEMBL389349 IC50 = 316.23 nM 6.50
CHEMBL389348 IC50 = 501.19 nM 6.30
CHEMBL228582 IC50 = 794.33 nM 6.10
CHEMBL394539 IC50 = 794.33 nM 6.10
CHEMBL228847 IC50 = 794.33 nM 6.10
CHEMBL228901 IC50 = 794.33 nM 6.10
CHEMBL387686 IC50 = 1584.89 nM 5.80
CHEMBL228635 IC50 = 3981.07 nM 5.40
CHEMBL390834 IC50 = 6309.57 nM 5.20
CHEMBL228900 IC50 = 50118.72 nM 4.30
CHEMBL228846 IC50 = 100000.0 nM 4.00