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Assay Detail

CHEMBL1068017

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Binding
Inhibition of L-type calcium channel alpha-1c/alpha-2-delta-1/beta-1b expressed in HEK293 cells by FLIPR method
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Publication

Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors.
Pajouhesh H, Feng ZP, Ding Y, Zhang L, Pajouhesh H, Morrison JL, Belardetti F, Tringham E, Simonson E, Vanderah TW, Porreca F, Zamponi GW, Mitscher LA, Snutch TP.
Bioorg Med Chem Lett (2010) 20 : 1378 -1383
PubMed 20117000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.44 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL605965 1 5.96
CHEMBL597969 1 5.96
CHEMBL598392 1 5.85
CHEMBL589285 1 5.85
CHEMBL606175 1 5.80
CHEMBL599408 1 5.80
CHEMBL597788 1 5.75
CHEMBL597970 1 5.60
CHEMBL598598 1 5.54
CHEMBL598603 1 5.54
CHEMBL597782 1 5.51
CHEMBL599217 1 5.46
CHEMBL599625 1 5.42
CHEMBL597585 1 5.21
CHEMBL599404 1 5.21
CHEMBL599403 1 5.17
CHEMBL599402 1 5.16
CHEMBL596946 1 5.13
CHEMBL597572 1 5.10
CHEMBL597775 1 5.07
CHEMBL605769 1 5.03
CHEMBL599015 1 5.02
CHEMBL598990 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL605965 IC50 = 1100.0 nM 5.96
CHEMBL597969 IC50 = 1100.0 nM 5.96
CHEMBL598392 IC50 = 1400.0 nM 5.85
CHEMBL589285 IC50 = 1400.0 nM 5.85
CHEMBL606175 IC50 = 1600.0 nM 5.80
CHEMBL599408 IC50 = 1600.0 nM 5.80
CHEMBL597788 IC50 = 1800.0 nM 5.75
CHEMBL597970 IC50 = 2500.0 nM 5.60
CHEMBL598598 IC50 = 2900.0 nM 5.54
CHEMBL598603 IC50 = 2900.0 nM 5.54
CHEMBL597782 IC50 = 3100.0 nM 5.51
CHEMBL599217 IC50 = 3500.0 nM 5.46
CHEMBL599625 IC50 = 3800.0 nM 5.42
CHEMBL597585 IC50 = 6100.0 nM 5.21
CHEMBL599404 IC50 = 6200.0 nM 5.21
CHEMBL599403 IC50 = 6800.0 nM 5.17
CHEMBL599402 IC50 = 6900.0 nM 5.16
CHEMBL596946 IC50 = 7400.0 nM 5.13
CHEMBL597572 IC50 = 7900.0 nM 5.10
CHEMBL597775 IC50 = 8600.0 nM 5.07
CHEMBL605769 IC50 = 9300.0 nM 5.03
CHEMBL599015 IC50 = 9600.0 nM 5.02
CHEMBL598990 IC50 = 10000.0 nM 5.00