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Assay Detail

CHEMBL3399050

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

Binding
Agonist activity at human recombinant DP1 receptor expressed in melanophores assessed as induction of pigment redistribution incubated for 90 mins
32
Total Activities
32
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

Prostaglandin D2 receptor (CHEMBL4427)
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
EC50 32 7.60 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3398215 1 8.77
CHEMBL3398219 1 8.52
CHEMBL3398212 1 8.22
CHEMBL3398220 1 7.96
CHEMBL3398208 1 7.77
CHEMBL3398237 1 7.68
CHEMBL3398206 1 7.68
CHEMBL3398221 1 7.62
CHEMBL3398209 1 7.60
CHEMBL3398227 1 7.51
CHEMBL3398218 1 7.51
CHEMBL3398228 1 7.44
CHEMBL3398229 1 7.40
CHEMBL3398235 1 7.38
CHEMBL3398210 1 7.36
CHEMBL3398236 1 7.32
CHEMBL3398223 1 7.32
CHEMBL3398211 1 7.21
CHEMBL3398224 1 7.06
CHEMBL3398222 1 6.75
CHEMBL3398226 1 -
CHEMBL3398225 1 -
CHEMBL3398217 1 -
CHEMBL3398216 1 -
CHEMBL3398230 1 -
CHEMBL3398231 1 -
CHEMBL3398232 1 -
CHEMBL3398233 1 -
CHEMBL3398234 1 -
CHEMBL3398214 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3398215 EC50 = 1.7 nM 8.77
CHEMBL3398219 EC50 = 3.0 nM 8.52
CHEMBL3398212 EC50 = 6.0 nM 8.22
CHEMBL3398220 EC50 = 11.0 nM 7.96
CHEMBL3398208 EC50 = 17.0 nM 7.77
CHEMBL3398237 EC50 = 21.0 nM 7.68
CHEMBL3398206 EC50 = 21.0 nM 7.68
CHEMBL3398221 EC50 = 24.0 nM 7.62
CHEMBL3398209 EC50 = 25.0 nM 7.60
CHEMBL3398227 EC50 = 31.0 nM 7.51
CHEMBL3398218 EC50 = 31.0 nM 7.51
CHEMBL3398228 EC50 = 36.0 nM 7.44
CHEMBL3398229 EC50 = 40.0 nM 7.40
CHEMBL3398235 EC50 = 42.0 nM 7.38
CHEMBL3398210 EC50 = 44.0 nM 7.36
CHEMBL3398223 EC50 = 48.0 nM 7.32
CHEMBL3398236 EC50 = 48.0 nM 7.32
CHEMBL3398211 EC50 = 61.0 nM 7.21
CHEMBL3398224 EC50 = 88.0 nM 7.06
CHEMBL3398222 EC50 = 180.0 nM 6.75
CHEMBL3398226 EC50 - -
CHEMBL3398225 EC50 - -
CHEMBL3398217 EC50 - -
CHEMBL3398216 EC50 - -
CHEMBL3398230 EC50 - -
CHEMBL3398231 EC50 - -
CHEMBL3398232 EC50 - -
CHEMBL3398233 EC50 - -
CHEMBL3398234 EC50 - -
CHEMBL3398214 EC50 - -
CHEMBL3398213 EC50 - -
CHEMBL3398207 EC50 - -