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Assay Detail

CHEMBL3399051

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

Binding
Agonist activity at human IP receptor in human platelets assessed as inhibition of ADP-induced platelet aggregation
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prostacyclin receptor (CHEMBL1995)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat.
Tran TA, Shin YJ, Kramer B, Choi J, Zou N, Vallar P, Martens P, Boatman PD, Adams JW, Ramirez J, Shi Y, Morgan M, Unett DJ, Chang S, Shu HH, Tung SF, Semple G.
Bioorg Med Chem Lett (2015) 25 : 1030 -1035
PubMed 25666818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.82 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3398235 1 7.21
CHEMBL3398236 1 7.21
CHEMBL3398229 1 7.19
CHEMBL3398228 1 7.06
CHEMBL3398224 1 6.72
CHEMBL3398227 1 6.66
CHEMBL3398232 1 6.64
CHEMBL3398237 1 6.54
CHEMBL3398222 1 6.49
CHEMBL3398233 1 6.48
CHEMBL3398223 1 -
CHEMBL3398225 1 -
CHEMBL3398226 1 -
CHEMBL3398230 1 -
CHEMBL3398231 1 -
CHEMBL3398234 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3398235 IC50 = 62.0 nM 7.21
CHEMBL3398236 IC50 = 62.0 nM 7.21
CHEMBL3398229 IC50 = 64.0 nM 7.19
CHEMBL3398228 IC50 = 87.0 nM 7.06
CHEMBL3398224 IC50 = 191.0 nM 6.72
CHEMBL3398227 IC50 = 220.0 nM 6.66
CHEMBL3398232 IC50 = 230.0 nM 6.64
CHEMBL3398237 IC50 = 288.0 nM 6.54
CHEMBL3398222 IC50 = 325.0 nM 6.49
CHEMBL3398233 IC50 = 330.0 nM 6.48
CHEMBL3398223 IC50 - -
CHEMBL3398225 IC50 - -
CHEMBL3398226 IC50 - -
CHEMBL3398230 IC50 - -
CHEMBL3398231 IC50 - -
CHEMBL3398234 IC50 - -