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Assay Detail

CHEMBL895361

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

Binding
Displacement of [125I]neurokinin A from human recombinant NK2 receptor
ChEMBL ↗
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Substance-K receptor (CHEMBL2327) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a new series of potent and selective linear tachykinin NK2 receptor antagonists.
Fedi V, Altamura M, Catalioto RM, Giannotti D, Giolitti A, Giuliani S, Guidi A, Harmat NJ, Lecci A, Meini S, Nannicini R, Pasqui F, Tramontana M, Triolo A, Maggi CA.
J Med Chem (2007) 50 : 4793 -4807
PubMed 17850056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 58 8.63 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL243711 — — 1 10.28
CHEMBL244362 — — 1 10.24
CHEMBL395972 — — 1 10.22
CHEMBL266125 IBODUTANT 3.0 1 10.12
CHEMBL395974 — — 1 10.01
CHEMBL242626 — — 1 9.93
CHEMBL394780 — — 1 9.88
CHEMBL395973 — — 1 9.85
CHEMBL243496 — — 1 9.65
CHEMBL395971 — — 1 9.63
CHEMBL244566 — — 1 9.55
CHEMBL395975 — — 1 9.43
CHEMBL389355 — — 1 9.37
CHEMBL243498 — — 1 9.26
CHEMBL242631 — — 1 9.18
CHEMBL230424 — — 1 9.12
CHEMBL394350 — — 1 9.12
CHEMBL2113292 — — 1 9.09
CHEMBL389744 — — 1 9.07
CHEMBL242619 — — 1 9.05
CHEMBL242625 — — 1 8.97
CHEMBL394607 — — 1 8.93
CHEMBL266108 — — 1 8.86
CHEMBL244364 — — 1 8.82
CHEMBL230324 — — 1 8.80
CHEMBL243497 — — 1 8.71
CHEMBL220365 — — 1 8.71
CHEMBL231173 — — 1 8.69
CHEMBL397264 — — 1 8.67
CHEMBL397263 — — 1 8.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL243711 — Ki = 0.05248 nM 10.28
CHEMBL244362 — Ki = 0.05754 nM 10.24
CHEMBL395972 — Ki = 0.06026 nM 10.22
CHEMBL266125 IBODUTANT Ki = 0.07586 nM 10.12
CHEMBL395974 — Ki = 0.09772 nM 10.01
CHEMBL242626 — Ki = 0.1175 nM 9.93
CHEMBL394780 — Ki = 0.1318 nM 9.88
CHEMBL395973 — Ki = 0.1413 nM 9.85
CHEMBL243496 — Ki = 0.2239 nM 9.65
CHEMBL395971 — Ki = 0.2344 nM 9.63
CHEMBL244566 — Ki = 0.2818 nM 9.55
CHEMBL395975 — Ki = 0.3715 nM 9.43
CHEMBL389355 — Ki = 0.4266 nM 9.37
CHEMBL243498 — Ki = 0.5495 nM 9.26
CHEMBL242631 — Ki = 0.6607 nM 9.18
CHEMBL230424 — Ki = 0.7586 nM 9.12
CHEMBL394350 — Ki = 0.7586 nM 9.12
CHEMBL2113292 — Ki = 0.8128 nM 9.09
CHEMBL389744 — Ki = 0.8511 nM 9.07
CHEMBL242619 — Ki = 0.8913 nM 9.05
CHEMBL242625 — Ki = 1.072 nM 8.97
CHEMBL394607 — Ki = 1.175 nM 8.93
CHEMBL266108 — Ki = 1.38 nM 8.86
CHEMBL244364 — Ki = 1.514 nM 8.82
CHEMBL230324 — Ki = 1.585 nM 8.80
CHEMBL243497 — Ki = 1.95 nM 8.71
CHEMBL220365 — Ki = 1.95 nM 8.71
CHEMBL231173 — Ki = 2.042 nM 8.69
CHEMBL397264 — Ki = 2.138 nM 8.67
CHEMBL397263 — Ki = 2.291 nM 8.64
CHEMBL230426 — Ki = 2.399 nM 8.62
CHEMBL244363 — Ki = 2.884 nM 8.54
CHEMBL428217 — Ki = 3.162 nM 8.50
CHEMBL395774 — Ki = 3.802 nM 8.42
CHEMBL243278 — Ki = 3.802 nM 8.42
CHEMBL243503 — Ki = 4.169 nM 8.38
CHEMBL242624 — Ki = 4.677 nM 8.33
CHEMBL244766 — Ki = 4.898 nM 8.31
CHEMBL389525 — Ki = 4.898 nM 8.31
CHEMBL397702 — Ki = 5.495 nM 8.26
CHEMBL437164 — Ki = 8.511 nM 8.07
CHEMBL243725 — Ki = 9.12 nM 8.04
CHEMBL394531 — Ki = 9.333 nM 8.03
CHEMBL390174 — Ki = 10.72 nM 7.97
CHEMBL231261 — Ki = 10.96 nM 7.96
CHEMBL243502 — Ki = 12.59 nM 7.90
CHEMBL243280 — Ki = 14.79 nM 7.83
CHEMBL242847 — Ki = 20.89 nM 7.68
CHEMBL243071 — Ki = 24.55 nM 7.61
CHEMBL230326 — Ki = 25.7 nM 7.59