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Assay Detail

CHEMBL954953

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

Functional
Antagonist activity at human adrenomedullin 2 receptor expressed in CHO cells assessed as effect on cAMP accumulation
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Adrenomedullin receptor, AM2; CALCRL/RAMP3 (CHEMBL2111191)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Miranda LP, Holder JR, Shi L, Bennett B, Aral J, Gegg CV, Wright M, Walker K, Doellgast G, Rogers R, Li H, Valladares V, Salyers K, Johnson E, Wild K.
J Med Chem (2008) 51 : 7889 -7897
PubMed 19053766 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.60 7.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL503773 1 7.93
CHEMBL509329 1 6.97
CHEMBL525571 1 6.58
CHEMBL525039 1 6.50
CHEMBL525810 1 6.43
CHEMBL509603 1 6.38
CHEMBL2372187 1 6.30
CHEMBL2372194 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL503773 IC50 = 11.8 nM 7.93
CHEMBL509329 IC50 = 108.0 nM 6.97
CHEMBL525571 IC50 = 266.0 nM 6.58
CHEMBL525039 IC50 = 318.0 nM 6.50
CHEMBL525810 IC50 = 375.0 nM 6.43
CHEMBL509603 IC50 = 418.0 nM 6.38
CHEMBL2372187 IC50 = 496.0 nM 6.30
CHEMBL2372194 IC50 = 2003.0 nM 5.70