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Assay Detail

CHEMBL645195

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

Functional
Antagonistic activity against rat aorta for affinity estimates representative of the Alpha-1D adrenergic receptor
ChEMBL ↗
63
Total Activities
63
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Aorta
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Alpha-1D adrenergic receptor (CHEMBL326) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.
Elworthy TR, Ford AP, Bantle GW, Morgans DJ, Ozer RS, Palmer WS, Repke DB, Romero M, Sandoval L, Sjogren EB, Talamás FX, Vazquez A, Wu H, Arredondo NF, Blue DR, DeSousa A, Gross LM, Kava MS, Lesnick JD, Vimont RL, Williams TJ, Zhu QM, Pfister JR, Clarke DE.
J Med Chem (1997) 40 : 2674 -2687
PubMed 9276013 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 61 7.35 8.70
pA2 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL433348 — — 1 8.70
CHEMBL93054 — — 1 8.50
CHEMBL313775 — — 1 8.40
CHEMBL92261 — — 1 8.20
CHEMBL313157 — — 1 8.10
CHEMBL327232 — — 1 8.00
CHEMBL88435 — — 1 8.00
CHEMBL91278 — — 1 8.00
CHEMBL88856 — — 1 8.00
CHEMBL92259 — — 1 8.00
CHEMBL90874 — — 1 8.00
CHEMBL88512 — — 1 8.00
CHEMBL314880 — — 1 7.90
CHEMBL88181 — — 1 7.90
CHEMBL312935 — — 1 7.80
CHEMBL90287 — — 1 7.80
CHEMBL330060 — — 1 7.80
CHEMBL330579 — — 1 7.80
CHEMBL89030 — — 1 7.70
CHEMBL91876 — — 1 7.70
CHEMBL329160 — — 1 7.70
CHEMBL327872 — — 1 7.70
CHEMBL327168 — — 1 7.60
CHEMBL91400 — — 1 7.50
CHEMBL90778 — — 1 7.50
CHEMBL329601 — — 1 7.50
CHEMBL91338 — — 1 7.50
CHEMBL91785 — — 1 7.40
CHEMBL92901 — — 1 7.40
CHEMBL91093 — — 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL433348 — Kd = 1.995 nM 8.70
CHEMBL93054 — Kd = 3.162 nM 8.50
CHEMBL313775 — Kd = 3.981 nM 8.40
CHEMBL92261 — Kd = 6.31 nM 8.20
CHEMBL313157 — Kd = 7.943 nM 8.10
CHEMBL327232 — Kd = 10.0 nM 8.00
CHEMBL88435 — Kd = 10.0 nM 8.00
CHEMBL91278 — Kd = 10.0 nM 8.00
CHEMBL88856 — Kd = 10.0 nM 8.00
CHEMBL92259 — Kd = 10.0 nM 8.00
CHEMBL90874 — Kd = 10.0 nM 8.00
CHEMBL88512 — Kd = 10.0 nM 8.00
CHEMBL88181 — Kd = 12.59 nM 7.90
CHEMBL314880 — Kd = 12.59 nM 7.90
CHEMBL330579 — Kd = 15.85 nM 7.80
CHEMBL312935 — Kd = 15.85 nM 7.80
CHEMBL330060 — Kd = 15.85 nM 7.80
CHEMBL90287 — Kd = 15.85 nM 7.80
CHEMBL89030 — Kd = 19.95 nM 7.70
CHEMBL91876 — Kd = 19.95 nM 7.70
CHEMBL329160 — Kd = 19.95 nM 7.70
CHEMBL327872 — Kd = 19.95 nM 7.70
CHEMBL327168 — Kd = 25.12 nM 7.60
CHEMBL91338 — Kd = 31.62 nM 7.50
CHEMBL329601 — Kd = 31.62 nM 7.50
CHEMBL91400 — Kd = 31.62 nM 7.50
CHEMBL90778 — Kd = 31.62 nM 7.50
CHEMBL91785 — Kd = 39.81 nM 7.40
CHEMBL92901 — Kd = 39.81 nM 7.40
CHEMBL91093 — Kd = 50.12 nM 7.30
CHEMBL88633 — Kd = 50.12 nM 7.30
CHEMBL93736 — Kd = 50.12 nM 7.30
CHEMBL90746 — Kd = 63.1 nM 7.20
CHEMBL88664 — Kd = 63.1 nM 7.20
CHEMBL88820 — Kd = 63.1 nM 7.20
CHEMBL91951 — Kd = 63.1 nM 7.20
CHEMBL91326 — Kd = 63.1 nM 7.20
CHEMBL88211 — Kd = 63.1 nM 7.20
CHEMBL420620 — Kd = 63.1 nM 7.20
CHEMBL90869 — Kd = 63.1 nM 7.20
CHEMBL89822 — Kd = 63.1 nM 7.20
CHEMBL328545 — Kd = 79.43 nM 7.10
CHEMBL315785 — Kd = 79.43 nM 7.10
CHEMBL90022 — Kd = 79.43 nM 7.10
CHEMBL327351 — Kd = 79.43 nM 7.10
CHEMBL91989 — Kd = 100.0 nM 7.00
CHEMBL91547 — Kd = 100.0 nM 7.00
CHEMBL91036 — Kd = 100.0 nM 7.00
CHEMBL90878 — Kd = 125.89 nM 6.90
CHEMBL88160 — Kd = 125.89 nM 6.90