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Assay Detail

CHEMBL5375217

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

Binding
Binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assay
12
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293-A
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G-protein coupled receptor 3 (CHEMBL4523856)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Fluorescent AF64394 Analogues Enables Real-Time Binding Studies for the Orphan Class A GPCR GPR3.
Bresinsky M, Shahraki A, Kolb P, Pockes S, Schihada H.
J Med Chem (2023) 66 : 15025 -15041
PubMed 37907069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 11 - -
Kd 1 6.99 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5410506 2 6.99
CHEMBL5423734 1 -
CHEMBL5394725 1 -
CHEMBL5405597 1 -
CHEMBL5414539 1 -
CHEMBL5420748 1 -
CHEMBL5398023 1 -
CHEMBL5401699 1 -
CHEMBL5427163 1 -
CHEMBL5396623 1 -
CHEMBL5421688 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5410506 Kd = 102.33 nM 6.99
CHEMBL5410506 Activity - -
CHEMBL5423734 Activity - -
CHEMBL5394725 Activity - -
CHEMBL5405597 Activity - -
CHEMBL5414539 Activity - -
CHEMBL5420748 Activity - -
CHEMBL5398023 Activity - -
CHEMBL5401699 Activity - -
CHEMBL5427163 Activity - -
CHEMBL5396623 Activity - -
CHEMBL5421688 Activity - -