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Assay Detail

CHEMBL772790

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

Functional
Calcium channel-blocking activity by determined by ability to antagonize calcium-induced contractions of isolated rabbit aortic strips
60
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 1 — Organism
Curated By Expert

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Synthesis, calcium-channel-blocking activity, and antihypertensive activity of 4-(diarylmethyl)-1-[3-(aryloxy)propyl]piperidines and structurally related compounds.
Shanklin JR, Johnson CP, Proakis AG, Barrett RJ.
J Med Chem (1991) 34 : 3011 -3022
PubMed 1920352 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 60 8.25 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193 NIFEDIPINE 4.0 1 9.80
CHEMBL322374 1 9.00
CHEMBL322419 1 8.90
CHEMBL102564 1 8.90
CHEMBL100902 1 8.90
CHEMBL319450 1 8.80
CHEMBL319018 1 8.80
CHEMBL100249 1 8.80
CHEMBL103777 1 8.70
CHEMBL100495 1 8.70
CHEMBL99677 1 8.70
CHEMBL102386 1 8.70
CHEMBL319807 1 8.60
CHEMBL103967 1 8.60
CHEMBL322220 1 8.60
CHEMBL318768 1 8.60
CHEMBL102696 1 8.60
CHEMBL103353 1 8.60
CHEMBL103608 1 8.60
CHEMBL17254 1 8.60
CHEMBL106495 1 8.60
CHEMBL103383 1 8.50
CHEMBL102549 1 8.50
CHEMBL105114 1 8.50
CHEMBL321093 1 8.50
CHEMBL105090 1 8.50
CHEMBL323560 1 8.40
CHEMBL317258 1 8.40
CHEMBL319491 1 8.30
CHEMBL103209 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193 NIFEDIPINE Kd = 0.1585 nM 9.80
CHEMBL322374 Kd = 1.0 nM 9.00
CHEMBL322419 Kd = 1.259 nM 8.90
CHEMBL102564 Kd = 1.259 nM 8.90
CHEMBL100902 Kd = 1.259 nM 8.90
CHEMBL319450 Kd = 1.585 nM 8.80
CHEMBL319018 Kd = 1.585 nM 8.80
CHEMBL100249 Kd = 1.585 nM 8.80
CHEMBL100495 Kd = 1.995 nM 8.70
CHEMBL99677 Kd = 1.995 nM 8.70
CHEMBL102386 Kd = 1.995 nM 8.70
CHEMBL103777 Kd = 1.995 nM 8.70
CHEMBL106495 Kd = 2.512 nM 8.60
CHEMBL17254 Kd = 2.512 nM 8.60
CHEMBL103608 Kd = 2.512 nM 8.60
CHEMBL318768 Kd = 2.512 nM 8.60
CHEMBL103353 Kd = 2.512 nM 8.60
CHEMBL102696 Kd = 2.512 nM 8.60
CHEMBL322220 Kd = 2.512 nM 8.60
CHEMBL103967 Kd = 2.512 nM 8.60
CHEMBL319807 Kd = 2.512 nM 8.60
CHEMBL105090 Kd = 3.162 nM 8.50
CHEMBL321093 Kd = 3.162 nM 8.50
CHEMBL102549 Kd = 3.162 nM 8.50
CHEMBL103383 Kd = 3.162 nM 8.50
CHEMBL105114 Kd = 3.162 nM 8.50
CHEMBL323560 Kd = 3.981 nM 8.40
CHEMBL317258 Kd = 3.981 nM 8.40
CHEMBL319491 Kd = 5.012 nM 8.30
CHEMBL103209 Kd = 5.012 nM 8.30
CHEMBL30008 FLUNARIZINE Kd = 5.012 nM 8.30
CHEMBL101086 Kd = 5.012 nM 8.30
CHEMBL105165 Kd = 6.31 nM 8.20
CHEMBL319619 Kd = 6.31 nM 8.20
CHEMBL102523 Kd = 6.31 nM 8.20
CHEMBL100074 Kd = 6.31 nM 8.20
CHEMBL273552 Kd = 6.31 nM 8.20
CHEMBL100304 Kd = 7.943 nM 8.10
CHEMBL318985 Kd = 7.943 nM 8.10
CHEMBL103830 Kd = 10.0 nM 8.00
CHEMBL321340 Kd = 10.0 nM 8.00
CHEMBL17436 Kd = 10.0 nM 8.00
CHEMBL321804 Kd = 10.0 nM 8.00
CHEMBL6966 VERAPAMIL Kd = 10.0 nM 8.00
CHEMBL420270 Kd = 12.59 nM 7.90
CHEMBL106496 Kd = 12.59 nM 7.90
CHEMBL103587 Kd = 12.59 nM 7.90
CHEMBL101346 Kd = 15.85 nM 7.80
CHEMBL101005 Kd = 15.85 nM 7.80
CHEMBL105534 Kd = 19.95 nM 7.70