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Assay Detail

CHEMBL1804405

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

Functional
Agonist activity at DYKDDDDK-flagged human GPR103 receptor expressed in CHO-K1 cells co-expressing G-protein alpha16 assessed as stimulation of calcium mobilization after 2 mins by fluorometric analysis
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Pyroglutamylated RF-amide peptide receptor (CHEMBL5852)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of a series of analogues of the RFamide-related peptide 26RFa.
Le Marec O, Neveu C, Lefranc B, Dubessy C, Boutin JA, Do-Régo JC, Costentin J, Tonon MC, Tena-Sempere M, Vaudry H, Leprince J.
J Med Chem (2011) 54 : 4806 -4814
PubMed 21623631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 6.38 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1802414 1 8.31
CHEMBL1802413 1 7.98
CHEMBL1802418 1 7.52
CHEMBL1802419 1 7.43
CHEMBL1802480 1 7.41
CHEMBL1800099 1 7.37
CHEMBL1802482 1 7.17
CHEMBL1802420 1 7.02
CHEMBL1802416 1 6.86
CHEMBL1802373 1 6.78
CHEMBL1802417 1 6.73
CHEMBL1802369 1 6.63
CHEMBL1802423 1 6.63
CHEMBL1802421 1 6.62
CHEMBL1802476 1 6.55
CHEMBL1802422 1 6.55
CHEMBL1802370 1 6.45
CHEMBL1802372 1 6.43
CHEMBL1802379 1 6.34
CHEMBL1802377 1 6.23
CHEMBL1802378 1 6.16
CHEMBL1802375 1 6.14
CHEMBL1802425 1 6.13
CHEMBL1802365 1 6.13
CHEMBL1802366 1 6.09
CHEMBL1802380 1 6.08
CHEMBL1802376 1 6.08
CHEMBL1802371 1 5.96
CHEMBL1802479 1 5.96
CHEMBL1802478 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1802414 EC50 = 4.9 nM 8.31
CHEMBL1802413 EC50 = 10.4 nM 7.98
CHEMBL1802418 EC50 = 30.2 nM 7.52
CHEMBL1802419 EC50 = 37.5 nM 7.43
CHEMBL1802480 EC50 = 39.0 nM 7.41
CHEMBL1800099 EC50 = 43.2 nM 7.37
CHEMBL1802482 EC50 = 67.0 nM 7.17
CHEMBL1802420 EC50 = 95.3 nM 7.02
CHEMBL1802416 EC50 = 138.0 nM 6.86
CHEMBL1802373 EC50 = 166.0 nM 6.78
CHEMBL1802417 EC50 = 185.0 nM 6.73
CHEMBL1802423 EC50 = 233.0 nM 6.63
CHEMBL1802369 EC50 = 233.0 nM 6.63
CHEMBL1802421 EC50 = 237.0 nM 6.62
CHEMBL1802422 EC50 = 282.0 nM 6.55
CHEMBL1802476 EC50 = 282.0 nM 6.55
CHEMBL1802370 EC50 = 355.0 nM 6.45
CHEMBL1802372 EC50 = 374.0 nM 6.43
CHEMBL1802379 EC50 = 455.0 nM 6.34
CHEMBL1802377 EC50 = 588.0 nM 6.23
CHEMBL1802378 EC50 = 695.0 nM 6.16
CHEMBL1802375 EC50 = 722.0 nM 6.14
CHEMBL1802365 EC50 = 741.0 nM 6.13
CHEMBL1802425 EC50 = 739.0 nM 6.13
CHEMBL1802366 EC50 = 817.0 nM 6.09
CHEMBL1802380 EC50 = 830.0 nM 6.08
CHEMBL1802376 EC50 = 826.0 nM 6.08
CHEMBL1802371 EC50 = 1103.0 nM 5.96
CHEMBL1802479 EC50 = 1088.0 nM 5.96
CHEMBL1802478 EC50 = 1198.0 nM 5.92
CHEMBL1802412 EC50 = 1308.0 nM 5.88
CHEMBL1802433 EC50 = 1333.0 nM 5.88
CHEMBL1802484 EC50 = 1443.0 nM 5.84
CHEMBL1802364 EC50 = 1471.0 nM 5.83
CHEMBL1802368 EC50 = 1631.0 nM 5.79
CHEMBL1802424 EC50 = 1710.0 nM 5.77
CHEMBL1802367 EC50 = 1820.0 nM 5.74
CHEMBL1802374 EC50 = 2545.0 nM 5.59
CHEMBL1802415 EC50 = 2910.0 nM 5.54
CHEMBL1802432 EC50 = 2985.0 nM 5.53
CHEMBL1802431 EC50 = 3350.0 nM 5.47
CHEMBL1802438 EC50 = 4975.0 nM 5.30