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Assay Detail

CHEMBL700076

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

Binding
Inhibition of [3H]D-888 binding to L-type [Ca2+] channel of membranes from rat skeletal muscle
33
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Muscle tissue
Confidence 9 — Direct single protein target
Curated By Expert

Target

Voltage-dependent L-type calcium channel subunit alpha-1S (CHEMBL4108)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New purines and purine analogs as modulators of multidrug resistance.
Dhainaut A, Regnier G, Tizot A, Pierre A, Leonce S, Guilbaud N, Kraus-Berthier L, Atassi G.
J Med Chem (1996) 39 : 4099 -4108
PubMed 8831775 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.69 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335742 1 8.30
CHEMBL334400 1 7.92
CHEMBL341462 1 7.34
CHEMBL134195 1 7.32
CHEMBL132844 1 7.21
CHEMBL130086 1 7.21
CHEMBL336375 1 7.08
CHEMBL338787 1 7.06
CHEMBL132000 1 7.05
CHEMBL85156 1 7.05
CHEMBL443810 1 7.03
CHEMBL336560 1 7.00
CHEMBL341438 1 6.96
CHEMBL130248 1 6.92
CHEMBL133118 1 6.77
CHEMBL132565 1 6.77
CHEMBL438385 1 6.70
CHEMBL133458 1 6.57
CHEMBL133062 1 6.40
CHEMBL336350 1 6.39
CHEMBL130301 1 6.38
CHEMBL337019 1 6.36
CHEMBL337682 1 6.31
CHEMBL132911 1 6.26
CHEMBL424637 1 6.25
CHEMBL133567 1 6.21
CHEMBL133781 1 6.20
CHEMBL340348 2 6.19
CHEMBL130484 1 6.11
CHEMBL131847 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335742 Ki = 5.0 nM 8.30
CHEMBL334400 Ki = 12.0 nM 7.92
CHEMBL341462 Ki = 46.0 nM 7.34
CHEMBL134195 Ki = 48.0 nM 7.32
CHEMBL132844 Ki = 62.0 nM 7.21
CHEMBL130086 Ki = 62.0 nM 7.21
CHEMBL336375 Ki = 84.0 nM 7.08
CHEMBL338787 Ki = 87.0 nM 7.06
CHEMBL132000 Ki = 90.0 nM 7.05
CHEMBL85156 Ki = 89.0 nM 7.05
CHEMBL443810 Ki = 93.0 nM 7.03
CHEMBL336560 Ki = 99.0 nM 7.00
CHEMBL341438 Ki = 110.0 nM 6.96
CHEMBL130248 Ki = 120.0 nM 6.92
CHEMBL132565 Ki = 170.0 nM 6.77
CHEMBL133118 Ki = 170.0 nM 6.77
CHEMBL438385 Ki = 200.0 nM 6.70
CHEMBL133458 Ki = 270.0 nM 6.57
CHEMBL133062 Ki = 400.0 nM 6.40
CHEMBL336350 Ki = 410.0 nM 6.39
CHEMBL130301 Ki = 420.0 nM 6.38
CHEMBL337019 Ki = 440.0 nM 6.36
CHEMBL337682 Ki = 490.0 nM 6.31
CHEMBL132911 Ki = 550.0 nM 6.26
CHEMBL424637 Ki = 560.0 nM 6.25
CHEMBL133567 Ki = 620.0 nM 6.21
CHEMBL133781 Ki = 630.0 nM 6.20
CHEMBL340348 Ki = 650.0 nM 6.19
CHEMBL130484 Ki = 770.0 nM 6.11
CHEMBL131847 Ki = 860.0 nM 6.07
CHEMBL340348 Ki = 1000.0 nM 6.00
CHEMBL132637 Ki = 1600.0 nM 5.80
CHEMBL132782 Ki = 3700.0 nM 5.43