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Assay Detail

CHEMBL2066643

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

Functional
Antagonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant compound preincubated for 10 mins by degranulation assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RBL-2H3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

De novo peptide design with C3a receptor agonist and antagonist activities: theoretical predictions and experimental validation.
Bellows-Peterson ML, Fung HK, Floudas CA, Kieslich CA, Zhang L, Morikis D, Wareham KJ, Monk PN, Hawksworth OA, Woodruff TM.
J Med Chem (2012) 55 : 4159 -4168
PubMed 22500977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.91 8.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064013 1 8.73
CHEMBL2064017 1 8.34
CHEMBL2064014 1 8.30
CHEMBL2064015 1 8.11
CHEMBL2064016 1 8.04
CHEMBL2064012 1 7.96
CHEMBL2064021 1 7.91
CHEMBL2064018 1 7.81
CHEMBL2064011 1 7.63
CHEMBL2064019 1 7.58
CHEMBL2063898 1 7.30
CHEMBL2064020 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064013 IC50 = 1.862 nM 8.73
CHEMBL2064017 IC50 = 4.571 nM 8.34
CHEMBL2064014 IC50 = 5.012 nM 8.30
CHEMBL2064015 IC50 = 7.762 nM 8.11
CHEMBL2064016 IC50 = 9.12 nM 8.04
CHEMBL2064012 IC50 = 10.96 nM 7.96
CHEMBL2064021 IC50 = 12.3 nM 7.91
CHEMBL2064018 IC50 = 15.49 nM 7.81
CHEMBL2064011 IC50 = 23.44 nM 7.63
CHEMBL2064019 IC50 = 26.3 nM 7.58
CHEMBL2063898 IC50 = 50.12 nM 7.30
CHEMBL2064020 IC50 = 63.1 nM 7.20