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Assay Detail

CHEMBL918150

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

Binding
Displacement of [125I]neurokinin A from human NK2 receptor expressed in CHOK1 cells
ChEMBL ↗
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Insertion of an aspartic acid moiety into cyclic pseudopeptides: synthesis and biological characterization of potent antagonists for the human Tachykinin NK-2 receptor.
Fedi V, Altamura M, Balacco G, Canfarini F, Criscuoli M, Giannotti D, Giolitti A, Giuliani S, Guidi A, Harmat NJ, Nannicini R, Pasqui F, Patacchini R, Perrotta E, Tramontana M, Triolo A, Maggi CA.
J Med Chem (2004) 47 : 6935 -6947
PubMed 15615542 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 9.27 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224081 — — 1 10.60
CHEMBL436981 — — 1 10.30
CHEMBL387506 — — 1 10.20
CHEMBL439281 — — 1 10.20
CHEMBL389510 — — 1 10.00
CHEMBL223221 — — 1 10.00
CHEMBL225297 — — 1 10.00
CHEMBL224003 — — 1 9.90
CHEMBL224374 — — 1 9.90
CHEMBL413715 — — 1 9.80
CHEMBL225588 — — 1 9.80
CHEMBL389459 — — 1 9.80
CHEMBL266284 — — 1 9.80
CHEMBL389511 — — 1 9.80
CHEMBL389279 — — 1 9.70
CHEMBL225392 — — 1 9.70
CHEMBL224009 — — 1 9.70
CHEMBL388626 — — 1 9.70
CHEMBL224494 — — 1 9.60
CHEMBL446450 — — 1 9.60
CHEMBL116812 — — 1 9.50
CHEMBL224426 — — 1 9.50
CHEMBL390168 — — 1 9.50
CHEMBL223993 — — 1 9.40
CHEMBL225475 — — 1 9.40
CHEMBL439377 — — 1 9.40
CHEMBL390167 — — 1 9.30
CHEMBL387542 — — 1 9.30
CHEMBL223994 — — 1 9.20
CHEMBL387698 — — 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224081 — Ki = 0.02512 nM 10.60
CHEMBL436981 — Ki = 0.05012 nM 10.30
CHEMBL439281 — Ki = 0.0631 nM 10.20
CHEMBL387506 — Ki = 0.0631 nM 10.20
CHEMBL389510 — Ki = 0.1 nM 10.00
CHEMBL223221 — Ki = 0.1 nM 10.00
CHEMBL225297 — Ki = 0.1 nM 10.00
CHEMBL224003 — Ki = 0.1259 nM 9.90
CHEMBL224374 — Ki = 0.1259 nM 9.90
CHEMBL389511 — Ki = 0.1585 nM 9.80
CHEMBL266284 — Ki = 0.1585 nM 9.80
CHEMBL389459 — Ki = 0.1585 nM 9.80
CHEMBL225588 — Ki = 0.1585 nM 9.80
CHEMBL413715 — Ki = 0.1585 nM 9.80
CHEMBL388626 — Ki = 0.1995 nM 9.70
CHEMBL389279 — Ki = 0.1995 nM 9.70
CHEMBL224009 — Ki = 0.1995 nM 9.70
CHEMBL225392 — Ki = 0.1995 nM 9.70
CHEMBL224494 — Ki = 0.2512 nM 9.60
CHEMBL446450 — Ki = 0.2512 nM 9.60
CHEMBL116812 — Ki = 0.3162 nM 9.50
CHEMBL224426 — Ki = 0.3162 nM 9.50
CHEMBL390168 — Ki = 0.3162 nM 9.50
CHEMBL439377 — Ki = 0.3981 nM 9.40
CHEMBL225475 — Ki = 0.3981 nM 9.40
CHEMBL223993 — Ki = 0.3981 nM 9.40
CHEMBL390167 — Ki = 0.5012 nM 9.30
CHEMBL387542 — Ki = 0.5012 nM 9.30
CHEMBL223994 — Ki = 0.631 nM 9.20
CHEMBL387698 — Ki = 0.7943 nM 9.10
CHEMBL224888 — Ki = 1.0 nM 9.00
CHEMBL436804 — Ki = 1.259 nM 8.90
CHEMBL387699 — Ki = 1.585 nM 8.80
CHEMBL375213 — Ki = 1.585 nM 8.80
CHEMBL224427 — Ki = 1.585 nM 8.80
CHEMBL223644 — Ki = 1.585 nM 8.80
CHEMBL224532 — Ki = 1.995 nM 8.70
CHEMBL435324 — Ki = 1.995 nM 8.70
CHEMBL376141 — Ki = 1.995 nM 8.70
CHEMBL420308 — Ki = 3.162 nM 8.50
CHEMBL387700 — Ki = 3.162 nM 8.50
CHEMBL438559 — Ki = 3.162 nM 8.50
CHEMBL225264 — Ki = 3.981 nM 8.40
CHEMBL389432 — Ki = 5.012 nM 8.30
CHEMBL438839 — Ki = 6.31 nM 8.20
CHEMBL225393 — Ki = 7.943 nM 8.10
CHEMBL375053 — Ki = 15.85 nM 7.80
CHEMBL375214 — Ki = 25.12 nM 7.60