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Assay Detail

CHEMBL649046

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Functional
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL ↗
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Alpha-1A adrenergic receptor (CHEMBL3637) ↗
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

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 8.74 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL314880 — — 1 10.70
CHEMBL313775 — — 1 10.00
CHEMBL330579 — — 1 10.00
CHEMBL327231 — — 1 9.90
CHEMBL91278 — — 1 9.80
CHEMBL836 TAMSULOSIN 4.0 1 9.80
CHEMBL91400 — — 1 9.70
CHEMBL327168 — — 1 9.50
CHEMBL88211 — — 1 9.40
CHEMBL313157 — — 1 9.30
CHEMBL88160 — — 1 9.30
CHEMBL433348 — — 1 9.30
CHEMBL315496 — — 1 9.30
CHEMBL89030 — — 1 9.30
CHEMBL315785 — — 1 9.20
CHEMBL91547 — — 1 9.20
CHEMBL329601 — — 1 9.20
CHEMBL91951 — — 1 9.20
CHEMBL327872 — — 1 9.10
CHEMBL90878 — — 1 9.10
CHEMBL329773 — — 1 9.10
CHEMBL91785 — — 1 9.10
CHEMBL330060 — — 1 9.00
CHEMBL93054 — — 1 9.00
CHEMBL89397 — — 1 8.90
CHEMBL90746 — — 1 8.90
CHEMBL90874 — — 1 8.90
CHEMBL91605 — — 1 8.90
CHEMBL90810 — — 1 8.90
CHEMBL90869 — — 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL314880 — Kd = 0.01995 nM 10.70
CHEMBL313775 — Kd = 0.1 nM 10.00
CHEMBL330579 — Kd = 0.1 nM 10.00
CHEMBL327231 — Kd = 0.1259 nM 9.90
CHEMBL91278 — Kd = 0.1585 nM 9.80
CHEMBL836 TAMSULOSIN Kd = 0.1585 nM 9.80
CHEMBL91400 — Kd = 0.1995 nM 9.70
CHEMBL327168 — Kd = 0.3162 nM 9.50
CHEMBL88211 — Kd = 0.3981 nM 9.40
CHEMBL89030 — Kd = 0.5012 nM 9.30
CHEMBL315496 — Kd = 0.5012 nM 9.30
CHEMBL433348 — Kd = 0.5012 nM 9.30
CHEMBL88160 — Kd = 0.5012 nM 9.30
CHEMBL313157 — Kd = 0.5012 nM 9.30
CHEMBL91951 — Kd = 0.631 nM 9.20
CHEMBL315785 — Kd = 0.631 nM 9.20
CHEMBL329601 — Kd = 0.631 nM 9.20
CHEMBL91547 — Kd = 0.631 nM 9.20
CHEMBL327872 — Kd = 0.7943 nM 9.10
CHEMBL90878 — Kd = 0.7943 nM 9.10
CHEMBL329773 — Kd = 0.7943 nM 9.10
CHEMBL91785 — Kd = 0.7943 nM 9.10
CHEMBL330060 — Kd = 1.0 nM 9.00
CHEMBL93054 — Kd = 1.0 nM 9.00
CHEMBL90746 — Kd = 1.259 nM 8.90
CHEMBL90810 — Kd = 1.259 nM 8.90
CHEMBL91605 — Kd = 1.259 nM 8.90
CHEMBL89397 — Kd = 1.259 nM 8.90
CHEMBL90874 — Kd = 1.259 nM 8.90
CHEMBL90869 — Kd = 1.585 nM 8.80
CHEMBL420620 — Kd = 1.585 nM 8.80
CHEMBL329160 — Kd = 1.585 nM 8.80
CHEMBL90022 — Kd = 1.585 nM 8.80
CHEMBL88181 — Kd = 1.995 nM 8.70
CHEMBL88435 — Kd = 1.995 nM 8.70
CHEMBL327232 — Kd = 1.995 nM 8.70
CHEMBL88856 — Kd = 1.995 nM 8.70
CHEMBL89822 — Kd = 2.512 nM 8.60
CHEMBL91326 — Kd = 3.162 nM 8.50
CHEMBL91036 — Kd = 3.162 nM 8.50
CHEMBL420060 — Kd = 3.981 nM 8.40
CHEMBL88633 — Kd = 3.981 nM 8.40
CHEMBL91338 — Kd = 3.981 nM 8.40
CHEMBL91989 — Kd = 3.981 nM 8.40
CHEMBL88664 — Kd = 5.012 nM 8.30
CHEMBL2 PRAZOSIN Kd = 5.012 nM 8.30
CHEMBL328545 — Kd = 6.31 nM 8.20
CHEMBL597 PHENTOLAMINE Kd = 6.31 nM 8.20
CHEMBL90287 — Kd = 6.31 nM 8.20
CHEMBL419867 — Kd = 7.943 nM 8.10