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Assay Detail

CHEMBL869276

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

Binding
Displacement of [125I]NDP-MSH from human MC4R expressed in HEK293 cells
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Arylpropionylpiperazines as antagonists of the human melanocortin-4 receptor.
Jiang W, Tucci FC, Chen CW, Arellano M, Tran JA, White NS, Marinkovic D, Pontillo J, Fleck BA, Wen J, Saunders J, Madan A, Foster AC, Chen C.
Bioorg Med Chem Lett (2006) 16 : 4674 -4678
PubMed 16777413 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 57 6.30 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL215659 1 7.89
CHEMBL212192 1 7.75
CHEMBL211564 1 7.72
CHEMBL215601 1 7.60
CHEMBL384636 1 7.52
CHEMBL212897 1 7.25
CHEMBL379625 1 7.24
CHEMBL214217 1 7.19
CHEMBL213738 1 7.13
CHEMBL213691 1 7.12
CHEMBL215886 1 7.07
CHEMBL209954 1 7.05
CHEMBL214000 1 7.04
CHEMBL213381 1 7.03
CHEMBL213380 1 6.96
CHEMBL213264 1 6.96
CHEMBL215851 1 6.85
CHEMBL213739 1 6.80
CHEMBL377480 1 6.77
CHEMBL215974 1 6.72
CHEMBL213953 1 6.68
CHEMBL214204 1 6.52
CHEMBL213041 1 6.46
CHEMBL212303 1 6.44
CHEMBL214988 1 6.40
CHEMBL384138 1 6.31
CHEMBL378397 1 6.21
CHEMBL384389 1 6.19
CHEMBL212889 1 6.16
CHEMBL215741 1 6.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL215659 Ki = 13.0 nM 7.89
CHEMBL212192 Ki = 18.0 nM 7.75
CHEMBL211564 Ki = 19.0 nM 7.72
CHEMBL215601 Ki = 25.0 nM 7.60
CHEMBL384636 Ki = 30.0 nM 7.52
CHEMBL212897 Ki = 56.0 nM 7.25
CHEMBL379625 Ki = 57.0 nM 7.24
CHEMBL214217 Ki = 64.0 nM 7.19
CHEMBL213738 Ki = 74.0 nM 7.13
CHEMBL213691 Ki = 75.0 nM 7.12
CHEMBL215886 Ki = 86.0 nM 7.07
CHEMBL209954 Ki = 89.0 nM 7.05
CHEMBL214000 Ki = 92.0 nM 7.04
CHEMBL213381 Ki = 94.0 nM 7.03
CHEMBL213264 Ki = 110.0 nM 6.96
CHEMBL213380 Ki = 110.0 nM 6.96
CHEMBL215851 Ki = 140.0 nM 6.85
CHEMBL213739 Ki = 160.0 nM 6.80
CHEMBL377480 Ki = 170.0 nM 6.77
CHEMBL215974 Ki = 190.0 nM 6.72
CHEMBL213953 Ki = 210.0 nM 6.68
CHEMBL214204 Ki = 300.0 nM 6.52
CHEMBL213041 Ki = 350.0 nM 6.46
CHEMBL212303 Ki = 360.0 nM 6.44
CHEMBL214988 Ki = 400.0 nM 6.40
CHEMBL384138 Ki = 490.0 nM 6.31
CHEMBL378397 Ki = 620.0 nM 6.21
CHEMBL384389 Ki = 640.0 nM 6.19
CHEMBL212889 Ki = 690.0 nM 6.16
CHEMBL215741 Ki = 780.0 nM 6.11
CHEMBL212653 Ki = 1000.0 nM 6.00
CHEMBL379792 Ki = 1400.0 nM 5.85
CHEMBL215697 Ki = 1500.0 nM 5.82
CHEMBL378016 Ki = 1600.0 nM 5.80
CHEMBL438793 Ki = 1700.0 nM 5.77
CHEMBL212553 Ki = 1800.0 nM 5.75
CHEMBL215712 Ki = 1900.0 nM 5.72
CHEMBL384040 Ki = 2100.0 nM 5.68
CHEMBL213776 Ki = 2200.0 nM 5.66
CHEMBL209869 Ki = 2300.0 nM 5.64
CHEMBL213935 Ki = 2400.0 nM 5.62
CHEMBL214537 Ki = 2500.0 nM 5.60
CHEMBL209682 Ki = 2500.0 nM 5.60
CHEMBL385437 Ki = 2600.0 nM 5.58
CHEMBL215646 Ki = 2600.0 nM 5.58
CHEMBL211462 Ki = 2800.0 nM 5.55
CHEMBL213389 Ki = 2800.0 nM 5.55
CHEMBL384390 Ki = 3000.0 nM 5.52
CHEMBL384965 Ki = 3300.0 nM 5.48
CHEMBL386868 Ki = 4000.0 nM 5.40