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Assay Detail

CHEMBL3737244

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

Binding
Displacement of ([125I]His3-MePhe7)-NKB from NK3 receptor (unknown origin) expressed in CHO cells by scintillation counter
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuromedin-K receptor (CHEMBL4429)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structureactivity relationship study on senktide for development of novel potent neurokinin-3 receptor selective agonists
Misu R, Yamamoto K, Yamada A, Noguchi T, Ohno H, Yamamura T, Okamura H, Matsuda F, Ohkura S, Oishi S, Fujii N
Medchemcomm (2015) 6 : 469 -476
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.78 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3734811 1 9.37
CHEMBL3736361 1 9.29
CHEMBL3736089 1 8.85
CHEMBL3735306 1 8.46
CHEMBL3735963 1 8.44
CHEMBL3736173 1 8.39
CHEMBL3735419 1 8.25
CHEMBL3735210 1 8.21
CHEMBL3734940 1 8.11
CHEMBL3736177 1 8.10
CHEMBL3734921 1 8.00
CHEMBL3735812 1 8.00
CHEMBL3735159 1 7.89
CHEMBL3736185 1 7.80
CHEMBL3735396 1 7.62
CHEMBL3735225 1 7.55
CHEMBL106124 SENKTIDE 1 7.54
CHEMBL3735400 1 7.47
CHEMBL3736512 1 7.43
CHEMBL3735427 1 7.41
CHEMBL3736299 1 7.26
CHEMBL3735951 1 7.17
CHEMBL3735858 1 7.17
CHEMBL3734932 1 7.14
CHEMBL3736459 1 7.08
CHEMBL3736198 1 7.04
CHEMBL3736227 1 6.98
CHEMBL3734892 1 6.91
CHEMBL3736313 1 6.76
CHEMBL3734931 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3734811 IC50 = 0.43 nM 9.37
CHEMBL3736361 IC50 = 0.51 nM 9.29
CHEMBL3736089 IC50 = 1.4 nM 8.85
CHEMBL3735306 IC50 = 3.5 nM 8.46
CHEMBL3735963 IC50 = 3.6 nM 8.44
CHEMBL3736173 IC50 = 4.1 nM 8.39
CHEMBL3735419 IC50 = 5.6 nM 8.25
CHEMBL3735210 IC50 = 6.1 nM 8.21
CHEMBL3734940 IC50 = 7.7 nM 8.11
CHEMBL3736177 IC50 = 7.9 nM 8.10
CHEMBL3734921 IC50 = 10.0 nM 8.00
CHEMBL3735812 IC50 = 9.9 nM 8.00
CHEMBL3735159 IC50 = 13.0 nM 7.89
CHEMBL3736185 IC50 = 16.0 nM 7.80
CHEMBL3735396 IC50 = 24.0 nM 7.62
CHEMBL3735225 IC50 = 28.0 nM 7.55
CHEMBL106124 SENKTIDE IC50 = 29.0 nM 7.54
CHEMBL3735400 IC50 = 34.0 nM 7.47
CHEMBL3736512 IC50 = 37.0 nM 7.43
CHEMBL3735427 IC50 = 39.0 nM 7.41
CHEMBL3736299 IC50 = 55.0 nM 7.26
CHEMBL3735951 IC50 = 68.0 nM 7.17
CHEMBL3735858 IC50 = 68.0 nM 7.17
CHEMBL3734932 IC50 = 73.0 nM 7.14
CHEMBL3736459 IC50 = 83.0 nM 7.08
CHEMBL3736198 IC50 = 91.0 nM 7.04
CHEMBL3736227 IC50 = 104.0 nM 6.98
CHEMBL3734892 IC50 = 123.0 nM 6.91
CHEMBL3736313 IC50 = 175.0 nM 6.76
CHEMBL3734931 IC50 > 10000.0 nM -
CHEMBL3735605 IC50 > 10000.0 nM -
CHEMBL3736383 IC50 > 10000.0 nM -