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Assay Detail

CHEMBL3405604

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

Binding
Displacement of [33P]-S1P from human S1P2 receptor expressed in CHOK1 cells after 60 mins by scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sphingosine 1-phosphate receptor 2 (CHEMBL2955)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.
Kusumi K, Shinozaki K, Kanaji T, Kurata H, Naganawa A, Otsuki K, Matsushita T, Sekiguchi T, Kakuuchi A, Seko T.
Bioorg Med Chem Lett (2015) 25 : 1479 -1482
PubMed 25746814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.06 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3401386 1 8.52
CHEMBL3401383 1 8.43
CHEMBL3401382 1 8.39
CHEMBL3401387 1 8.06
CHEMBL3401384 1 7.89
CHEMBL3401381 1 7.35
CHEMBL3401388 1 7.35
CHEMBL3401385 1 7.31
CHEMBL3401390 1 6.41
CHEMBL3401376 1 6.30
CHEMBL3401377 1 6.07
CHEMBL3401389 1 6.03
CHEMBL3401379 1 6.01
CHEMBL3401375 1 5.92
CHEMBL3401378 1 5.85
CHEMBL3401380 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3401386 IC50 = 3.0 nM 8.52
CHEMBL3401383 IC50 = 3.7 nM 8.43
CHEMBL3401382 IC50 = 4.1 nM 8.39
CHEMBL3401387 IC50 = 8.8 nM 8.06
CHEMBL3401384 IC50 = 13.0 nM 7.89
CHEMBL3401381 IC50 = 45.0 nM 7.35
CHEMBL3401388 IC50 = 45.0 nM 7.35
CHEMBL3401385 IC50 = 49.0 nM 7.31
CHEMBL3401390 IC50 = 390.0 nM 6.41
CHEMBL3401376 IC50 = 500.0 nM 6.30
CHEMBL3401377 IC50 = 860.0 nM 6.07
CHEMBL3401389 IC50 = 940.0 nM 6.03
CHEMBL3401379 IC50 = 980.0 nM 6.01
CHEMBL3401375 IC50 = 1200.0 nM 5.92
CHEMBL3401378 IC50 = 1400.0 nM 5.85
CHEMBL3401380 IC50 - -