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Assay Detail

CHEMBL3266750

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Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Apelin receptor (CHEMBL1628481)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identifying structural determinants of potency for analogs of apelin-13: integration of C-terminal truncation with structure-activity.
Zhang Y, Maitra R, Harris DL, Dhungana S, Snyder R, Runyon SP.
Bioorg Med Chem (2014) 22 : 2992 -2997
PubMed 24755525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 33 7.51 9.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3184840 1 9.38
CHEMBL414173 1 9.06
CHEMBL3261778 1 8.96
CHEMBL3261787 1 8.77
CHEMBL3261776 1 8.72
CHEMBL3261789 1 8.66
CHEMBL3261786 1 8.49
CHEMBL3261773 1 8.36
CHEMBL3261774 1 8.33
CHEMBL3261780 1 8.05
CHEMBL3261767 1 7.72
CHEMBL3261766 1 7.70
CHEMBL3261779 1 7.51
CHEMBL3262012 1 7.48
CHEMBL3261788 1 7.36
CHEMBL3261790 1 7.14
CHEMBL3262016 1 7.08
CHEMBL3261783 1 6.62
CHEMBL3261784 1 6.31
CHEMBL3262011 1 6.27
CHEMBL3261782 1 6.20
CHEMBL3261775 1 6.16
CHEMBL3261781 1 6.03
CHEMBL3261777 1 5.86
CHEMBL3261768 1 5.63
CHEMBL3261769 1 -
CHEMBL3261770 1 -
CHEMBL3261771 1 -
CHEMBL3261772 1 -
CHEMBL3261785 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3184840 EC50 = 0.42 nM 9.38
CHEMBL414173 EC50 = 0.87 nM 9.06
CHEMBL3261778 EC50 = 1.1 nM 8.96
CHEMBL3261787 EC50 = 1.7 nM 8.77
CHEMBL3261776 EC50 = 1.9 nM 8.72
CHEMBL3261789 EC50 = 2.2 nM 8.66
CHEMBL3261786 EC50 = 3.2 nM 8.49
CHEMBL3261773 EC50 = 4.4 nM 8.36
CHEMBL3261774 EC50 = 4.7 nM 8.33
CHEMBL3261780 EC50 = 8.9 nM 8.05
CHEMBL3261767 EC50 = 19.0 nM 7.72
CHEMBL3261766 EC50 = 20.0 nM 7.70
CHEMBL3261779 EC50 = 31.0 nM 7.51
CHEMBL3262012 EC50 = 33.0 nM 7.48
CHEMBL3261788 EC50 = 44.0 nM 7.36
CHEMBL3261790 EC50 = 73.0 nM 7.14
CHEMBL3262016 EC50 = 83.18 nM 7.08
CHEMBL3261783 EC50 = 237.0 nM 6.62
CHEMBL3261784 EC50 = 494.0 nM 6.31
CHEMBL3262011 EC50 = 539.0 nM 6.27
CHEMBL3261782 EC50 = 637.0 nM 6.20
CHEMBL3261775 EC50 = 691.0 nM 6.16
CHEMBL3261781 EC50 = 936.0 nM 6.03
CHEMBL3261777 EC50 = 1383.0 nM 5.86
CHEMBL3261768 EC50 = 2350.0 nM 5.63
CHEMBL3261769 EC50 > 3000.0 nM -
CHEMBL3261770 EC50 > 3000.0 nM -
CHEMBL3261771 EC50 > 3000.0 nM -
CHEMBL3261772 EC50 > 3000.0 nM -
CHEMBL3261785 EC50 > 3000.0 nM -
CHEMBL3262013 EC50 > 3000.0 nM -
CHEMBL3262015 EC50 > 31622.78 nM -
CHEMBL3262014 EC50 > 31622.78 nM -