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Assay Detail

CHEMBL859403

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Functional
pA2 value was calculated from dose-response plots generated by using different concentrations ranging between 1 and 10 uM antagonist.
10
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Adenylate cyclase type 5 (CHEMBL3189)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences.
Azizeh BY, Shenderovich MD, Trivedi D, Li G, Sturm NS, Hruby VJ.
J Med Chem (1996) 39 : 2449 -2455
PubMed 8691441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 10 6.29 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2115191 1 6.85
CHEMBL413666 1 6.60
CHEMBL2369127 1 6.50
CHEMBL328942 3 6.20
CHEMBL3037804 1 6.20
CHEMBL2114177 1 6.20
CHEMBL2114176 1 6.20
CHEMBL2115192 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2115191 Kd = 141.25 nM 6.85
CHEMBL413666 Kd = 251.19 nM 6.60
CHEMBL2369127 Kd = 316.23 nM 6.50
CHEMBL3037804 Kd = 630.96 nM 6.20
CHEMBL328942 Kd = 630.96 nM 6.20
CHEMBL2114177 Kd = 630.96 nM 6.20
CHEMBL2114176 Kd = 630.96 nM 6.20
CHEMBL328942 Kd = 707.95 nM 6.15
CHEMBL328942 Kd = 794.33 nM 6.10
CHEMBL2115192 Kd = 1412.54 nM 5.85