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Assay Detail

CHEMBL814715

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

Binding
Functional potency against Tachykinin receptor 2 (NK2) in rabbit pulmonary artery assay
ChEMBL ↗
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Tissue Artery
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Substance-P receptor (CHEMBL249) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)- 5-[2-[(3-substituted)-1-azetidinyl]ethyl]-2-piperidones. 1. Selective antagonists of the neurokinin-2 receptor.
MacKenzie AR, Marchington AP, Middleton DS, Newman SD, Jones BC.
J Med Chem (2002) 45 : 5365 -5377
PubMed 12431064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 43 8.60 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL151177 — — 1 10.10
CHEMBL151585 — — 1 9.90
CHEMBL71397 — — 1 9.50
CHEMBL149794 — — 1 9.40
CHEMBL150709 — — 1 9.30
CHEMBL149690 — — 1 9.30
CHEMBL348653 — — 1 9.30
CHEMBL151231 — — 1 9.20
CHEMBL150619 — — 1 9.20
CHEMBL423584 — — 1 9.20
CHEMBL151317 — — 1 9.00
CHEMBL185572 — — 1 9.00
CHEMBL150842 — — 1 8.90
CHEMBL151570 — — 1 8.90
CHEMBL150997 — — 1 8.90
CHEMBL148998 — — 1 8.90
CHEMBL151088 — — 1 8.80
CHEMBL151289 — — 1 8.80
CHEMBL150537 — — 1 8.70
CHEMBL345309 — — 1 8.70
CHEMBL358418 — — 1 8.70
CHEMBL150585 — — 1 8.70
CHEMBL151155 — — 1 8.60
CHEMBL347284 — — 1 8.60
CHEMBL150381 — — 1 8.50
CHEMBL357357 — — 1 8.50
CHEMBL151356 — — 1 8.50
CHEMBL345733 — — 1 8.50
CHEMBL151028 — — 1 8.30
CHEMBL355973 — — 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL151177 — Kd = 0.07943 nM 10.10
CHEMBL151585 — Kd = 0.1259 nM 9.90
CHEMBL71397 — Kd = 0.3162 nM 9.50
CHEMBL149794 — Kd = 0.3981 nM 9.40
CHEMBL150709 — Kd = 0.5012 nM 9.30
CHEMBL149690 — Kd = 0.5012 nM 9.30
CHEMBL348653 — Kd = 0.5012 nM 9.30
CHEMBL151231 — Kd = 0.631 nM 9.20
CHEMBL150619 — Kd = 0.631 nM 9.20
CHEMBL423584 — Kd = 0.631 nM 9.20
CHEMBL151317 — Kd = 1.0 nM 9.00
CHEMBL185572 — Kd = 1.0 nM 9.00
CHEMBL148998 — Kd = 1.259 nM 8.90
CHEMBL150997 — Kd = 1.259 nM 8.90
CHEMBL151570 — Kd = 1.259 nM 8.90
CHEMBL150842 — Kd = 1.259 nM 8.90
CHEMBL151088 — Kd = 1.585 nM 8.80
CHEMBL151289 — Kd = 1.585 nM 8.80
CHEMBL150585 — Kd = 1.995 nM 8.70
CHEMBL358418 — Kd = 1.995 nM 8.70
CHEMBL150537 — Kd = 1.995 nM 8.70
CHEMBL345309 — Kd = 1.995 nM 8.70
CHEMBL151155 — Kd = 2.512 nM 8.60
CHEMBL347284 — Kd = 2.512 nM 8.60
CHEMBL150381 — Kd = 3.162 nM 8.50
CHEMBL357357 — Kd = 3.162 nM 8.50
CHEMBL151356 — Kd = 3.162 nM 8.50
CHEMBL345733 — Kd = 3.162 nM 8.50
CHEMBL151028 — Kd = 5.012 nM 8.30
CHEMBL355973 — Kd = 5.012 nM 8.30
CHEMBL151288 — Kd = 6.31 nM 8.20
CHEMBL150644 — Kd = 6.31 nM 8.20
CHEMBL358694 — Kd = 7.943 nM 8.10
CHEMBL345288 — Kd = 10.0 nM 8.00
CHEMBL147301 — Kd = 10.0 nM 8.00
CHEMBL357946 — Kd = 10.0 nM 8.00
CHEMBL149469 — Kd = 12.59 nM 7.90
CHEMBL147241 — Kd = 15.85 nM 7.80
CHEMBL151026 — Kd = 15.85 nM 7.80
CHEMBL358600 — Kd = 19.95 nM 7.70
CHEMBL151621 — Kd = 100.0 nM 7.00
CHEMBL2111193 — Kd = 630.96 nM 6.20
CHEMBL151500 — Kd > 10000.0 nM -