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Assay Detail

CHEMBL864259

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

Binding
Displacement of [3H]PGE2 from EP1 receptor expressed in CHO-K1 cells
28
Total Activities
28
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 Expert

Target

Prostaglandin E2 receptor EP1 subtype (CHEMBL1811)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of novel pyrazole acid antagonists for the EP1 receptor.
McKeown SC, Hall A, Giblin GM, Lorthioir O, Blunt R, Lewell XQ, Wilson RJ, Brown SH, Chowdhury A, Coleman T, Watson SP, Chessell IP, Pipe A, Clayton N, Goldsmith P.
Bioorg Med Chem Lett (2006) 16 : 4767 -4771
PubMed 16843659 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.24 9.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214971 1 9.88
CHEMBL214967 1 9.28
CHEMBL402880 1 8.50
CHEMBL362543 1 8.45
CHEMBL213221 1 8.19
CHEMBL215453 1 8.13
CHEMBL215400 1 8.06
CHEMBL213412 1 8.01
CHEMBL215573 1 7.83
CHEMBL387454 1 7.75
CHEMBL215956 1 7.45
CHEMBL215667 1 6.94
CHEMBL213669 1 6.91
CHEMBL212667 1 6.90
CHEMBL214900 1 6.71
CHEMBL425076 1 6.51
CHEMBL385620 1 6.45
CHEMBL380297 1 6.37
CHEMBL215690 1 6.34
CHEMBL215687 1 6.24
CHEMBL214639 1 6.17
CHEMBL386532 1 5.91
CHEMBL378197 1 5.59
CHEMBL378533 1 5.28
CHEMBL215992 1 -
CHEMBL214914 1 -
CHEMBL213875 1 -
CHEMBL384332 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214971 IC50 = 0.1318 nM 9.88
CHEMBL214967 IC50 = 0.5248 nM 9.28
CHEMBL402880 IC50 = 3.162 nM 8.50
CHEMBL362543 IC50 = 3.548 nM 8.45
CHEMBL213221 IC50 = 6.457 nM 8.19
CHEMBL215453 IC50 = 7.413 nM 8.13
CHEMBL215400 IC50 = 8.71 nM 8.06
CHEMBL213412 IC50 = 9.772 nM 8.01
CHEMBL215573 IC50 = 14.79 nM 7.83
CHEMBL387454 IC50 = 17.78 nM 7.75
CHEMBL215956 IC50 = 35.48 nM 7.45
CHEMBL215667 IC50 = 114.82 nM 6.94
CHEMBL213669 IC50 = 123.03 nM 6.91
CHEMBL212667 IC50 = 125.89 nM 6.90
CHEMBL214900 IC50 = 194.98 nM 6.71
CHEMBL425076 IC50 = 309.03 nM 6.51
CHEMBL385620 IC50 = 354.81 nM 6.45
CHEMBL380297 IC50 = 426.58 nM 6.37
CHEMBL215690 IC50 = 457.09 nM 6.34
CHEMBL215687 IC50 = 575.44 nM 6.24
CHEMBL214639 IC50 = 676.08 nM 6.17
CHEMBL386532 IC50 = 1230.27 nM 5.91
CHEMBL378197 IC50 = 2570.4 nM 5.59
CHEMBL378533 IC50 = 5248.07 nM 5.28
CHEMBL215992 IC50 < 1995.26 nM -
CHEMBL214914 IC50 < 1995.26 nM -
CHEMBL213875 IC50 < 1995.26 nM -
CHEMBL384332 IC50 < 1995.26 nM -