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Assay Detail

CHEMBL1069758

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Functional
Antagonist activity at human CRTH2 receptor expressed in HEK285-7 cells assessed as inhibition of beta arrestin translocation by bioluminescence resonance energy transfer assay
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK285-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin D2 receptor 2 (CHEMBL5071) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel selective thiazoleacetic acids as CRTH2 antagonists developed from in silico derived hits. Part 1.
Rist Ø, Grimstrup M, Receveur JM, Frimurer TM, Ulven T, Kostenis E, Högberg T.
Bioorg Med Chem Lett (2010) 20 : 1177 -1180
PubMed 20031403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 6.12 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603659 — — 1 7.42
CHEMBL603158 — — 1 7.18
CHEMBL590090 — — 1 7.03
CHEMBL590395 — — 1 6.80
CHEMBL602925 — — 1 6.75
CHEMBL592217 — — 1 6.72
CHEMBL605351 — — 1 6.66
CHEMBL603658 — — 1 6.58
CHEMBL592458 — — 1 6.57
CHEMBL596712 — — 1 6.46
CHEMBL605138 — — 1 6.43
CHEMBL601621 — — 1 6.43
CHEMBL600475 — — 1 6.41
CHEMBL601278 — — 1 6.33
CHEMBL597725 — — 1 6.32
CHEMBL607423 — — 1 6.29
CHEMBL596915 — — 1 6.27
CHEMBL589092 FENTIAZAC 2.0 1 6.26
CHEMBL599784 — — 1 6.25
CHEMBL589502 — — 1 6.24
CHEMBL599176 — — 1 6.24
CHEMBL599879 — — 1 6.14
CHEMBL600261 — — 1 6.09
CHEMBL599177 — — 1 6.07
CHEMBL603949 — — 1 6.07
CHEMBL592001 — — 1 6.06
CHEMBL596728 — — 1 6.00
CHEMBL597118 — — 1 5.96
CHEMBL602386 — — 1 5.92
CHEMBL596727 — — 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603659 — IC50 = 38.0 nM 7.42
CHEMBL603158 — IC50 = 66.0 nM 7.18
CHEMBL590090 — IC50 = 93.0 nM 7.03
CHEMBL590395 — IC50 = 160.0 nM 6.80
CHEMBL602925 — IC50 = 180.0 nM 6.75
CHEMBL592217 — IC50 = 190.0 nM 6.72
CHEMBL605351 — IC50 = 220.0 nM 6.66
CHEMBL603658 — IC50 = 260.0 nM 6.58
CHEMBL592458 — IC50 = 270.0 nM 6.57
CHEMBL596712 — IC50 = 350.0 nM 6.46
CHEMBL605138 — IC50 = 370.0 nM 6.43
CHEMBL601621 — IC50 = 370.0 nM 6.43
CHEMBL600475 — IC50 = 390.0 nM 6.41
CHEMBL601278 — IC50 = 470.0 nM 6.33
CHEMBL597725 — IC50 = 480.0 nM 6.32
CHEMBL607423 — IC50 = 510.0 nM 6.29
CHEMBL596915 — IC50 = 540.0 nM 6.27
CHEMBL589092 FENTIAZAC IC50 = 550.0 nM 6.26
CHEMBL599784 — IC50 = 560.0 nM 6.25
CHEMBL589502 — IC50 = 570.0 nM 6.24
CHEMBL599176 — IC50 = 580.0 nM 6.24
CHEMBL599879 — IC50 = 730.0 nM 6.14
CHEMBL600261 — IC50 = 820.0 nM 6.09
CHEMBL599177 — IC50 = 850.0 nM 6.07
CHEMBL603949 — IC50 = 860.0 nM 6.07
CHEMBL592001 — IC50 = 870.0 nM 6.06
CHEMBL596728 — IC50 = 990.0 nM 6.00
CHEMBL597118 — IC50 = 1100.0 nM 5.96
CHEMBL602386 — IC50 = 1200.0 nM 5.92
CHEMBL596727 — IC50 = 1300.0 nM 5.89
CHEMBL600477 — IC50 = 1300.0 nM 5.89
CHEMBL591519 — IC50 = 1300.0 nM 5.89
CHEMBL596711 — IC50 = 1500.0 nM 5.82
CHEMBL596627 — IC50 = 1500.0 nM 5.82
CHEMBL590397 — IC50 = 1500.0 nM 5.82
CHEMBL602322 — IC50 = 1500.0 nM 5.82
CHEMBL600040 — IC50 = 1800.0 nM 5.75
CHEMBL596911 — IC50 = 1900.0 nM 5.72
CHEMBL597524 — IC50 = 1900.0 nM 5.72
CHEMBL597108 — IC50 = 2100.0 nM 5.68
CHEMBL609898 — IC50 = 2400.0 nM 5.62
CHEMBL590309 — IC50 = 3800.0 nM 5.42
CHEMBL603869 — IC50 = 3800.0 nM 5.42
CHEMBL591984 — IC50 = 4100.0 nM 5.39
CHEMBL590965 — IC50 = 7000.0 nM 5.16
CHEMBL605149 — IC50 = 16000.0 nM 4.80
CHEMBL591517 — IC50 > 100000.0 nM -
CHEMBL591042 — IC50 > 100000.0 nM -
CHEMBL591516 — IC50 > 100000.0 nM -
CHEMBL603187 — IC50 > 100000.0 nM -