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Assay Detail

CHEMBL5145224

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

Binding
Agonist activity at rabbit GPR38 expressed in COS-7 cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Cell Type COS-7
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
Toda N, Shida T, Takano R, Katagiri T, Hirouchi M, Abe M, Soma K, Nakagami Y, Yamazaki M.
Bioorg Med Chem Lett (2022) 59 : 128554 -128554
PubMed 35051575 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 8.92 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5179573 1 9.89
CHEMBL525634 1 9.80
CHEMBL5179543 1 9.74
CHEMBL5187928 1 9.68
CHEMBL5192530 1 9.59
CHEMBL5184722 1 9.59
CHEMBL5196982 1 9.29
CHEMBL5190786 1 9.21
CHEMBL5203126 1 9.00
CHEMBL5171964 1 8.96
CHEMBL5196819 1 8.92
CHEMBL5179463 1 8.89
CHEMBL5201797 1 8.89
CHEMBL5175905 1 8.77
CHEMBL5197045 1 8.59
CHEMBL465925 1 8.42
CHEMBL489095 CAMICINAL 3.0 1 7.38
CHEMBL5181246 1 5.89
CHEMBL5192584 1 -
CHEMBL5179060 1 -
CHEMBL5187776 1 -
CHEMBL5187975 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5179573 EC50 = 0.13 nM 9.89
CHEMBL525634 EC50 = 0.16 nM 9.80
CHEMBL5179543 EC50 = 0.18 nM 9.74
CHEMBL5187928 EC50 = 0.21 nM 9.68
CHEMBL5192530 EC50 = 0.26 nM 9.59
CHEMBL5184722 EC50 = 0.26 nM 9.59
CHEMBL5196982 EC50 = 0.51 nM 9.29
CHEMBL5190786 EC50 = 0.62 nM 9.21
CHEMBL5203126 EC50 = 1.0 nM 9.00
CHEMBL5171964 EC50 = 1.1 nM 8.96
CHEMBL5196819 EC50 = 1.2 nM 8.92
CHEMBL5179463 EC50 = 1.3 nM 8.89
CHEMBL5201797 EC50 = 1.3 nM 8.89
CHEMBL5175905 EC50 = 1.7 nM 8.77
CHEMBL5197045 EC50 = 2.6 nM 8.59
CHEMBL465925 EC50 = 3.8 nM 8.42
CHEMBL489095 CAMICINAL EC50 = 42.0 nM 7.38
CHEMBL5181246 EC50 = 1300.0 nM 5.89
CHEMBL5192584 EC50 - -
CHEMBL5179060 EC50 - -
CHEMBL5187776 EC50 - -
CHEMBL5187975 EC50 > 10000.0 nM -