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Assay Detail

CHEMBL1068015

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

Binding
Inhibition of N type calcium channel alpha-1b/alpha-2-delta-1/beta-1b expressed in HEK293 cells at holding potential of -100 mV by whole-cell patch clamp method
ChEMBL ↗
50
Total Activities
50
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

Target

N-type calcium channel alpha-1b/alpha2delta-1/beta-1b (CHEMBL4106160) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

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 50 6.57 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL599404 — — 1 7.40
CHEMBL597782 — — 1 7.40
CHEMBL599402 — — 1 7.30
CHEMBL605965 — — 1 7.30
CHEMBL599829 — — 1 7.22
CHEMBL597585 — — 1 7.16
CHEMBL598592 — — 1 7.05
CHEMBL597783 — — 1 7.00
CHEMBL604710 Z160 2.0 1 6.96
CHEMBL597788 — — 1 6.96
CHEMBL596946 — — 1 6.96
CHEMBL598598 — — 1 6.96
CHEMBL599821 — — 1 6.85
CHEMBL599403 — — 1 6.85
CHEMBL599217 — — 1 6.82
CHEMBL598806 — — 1 6.77
CHEMBL603465 — — 1 6.75
CHEMBL597957 — — 1 6.70
CHEMBL604298 — — 1 6.68
CHEMBL599016 — — 1 6.68
CHEMBL599832 — — 1 6.66
CHEMBL599015 — — 1 6.64
CHEMBL597572 — — 1 6.62
CHEMBL598603 — — 1 6.62
CHEMBL606175 — — 1 6.60
CHEMBL599205 — — 1 6.58
CHEMBL599408 — — 1 6.58
CHEMBL605769 — — 1 6.57
CHEMBL597757 — — 1 6.55
CHEMBL598793 — — 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL599404 — IC50 = 40.0 nM 7.40
CHEMBL597782 — IC50 = 40.0 nM 7.40
CHEMBL605965 — IC50 = 50.0 nM 7.30
CHEMBL599402 — IC50 = 50.0 nM 7.30
CHEMBL599829 — IC50 = 60.0 nM 7.22
CHEMBL597585 — IC50 = 70.0 nM 7.16
CHEMBL598592 — IC50 = 90.0 nM 7.05
CHEMBL597783 — IC50 = 100.0 nM 7.00
CHEMBL604710 Z160 IC50 = 110.0 nM 6.96
CHEMBL597788 — IC50 = 110.0 nM 6.96
CHEMBL596946 — IC50 = 110.0 nM 6.96
CHEMBL598598 — IC50 = 110.0 nM 6.96
CHEMBL599821 — IC50 = 140.0 nM 6.85
CHEMBL599403 — IC50 = 140.0 nM 6.85
CHEMBL599217 — IC50 = 150.0 nM 6.82
CHEMBL598806 — IC50 = 170.0 nM 6.77
CHEMBL603465 — IC50 = 180.0 nM 6.75
CHEMBL597957 — IC50 = 200.0 nM 6.70
CHEMBL604298 — IC50 = 210.0 nM 6.68
CHEMBL599016 — IC50 = 210.0 nM 6.68
CHEMBL599832 — IC50 = 220.0 nM 6.66
CHEMBL599015 — IC50 = 230.0 nM 6.64
CHEMBL597572 — IC50 = 240.0 nM 6.62
CHEMBL598603 — IC50 = 240.0 nM 6.62
CHEMBL606175 — IC50 = 250.0 nM 6.60
CHEMBL599205 — IC50 = 260.0 nM 6.58
CHEMBL599408 — IC50 = 260.0 nM 6.58
CHEMBL605769 — IC50 = 270.0 nM 6.57
CHEMBL597757 — IC50 = 280.0 nM 6.55
CHEMBL598793 — IC50 = 280.0 nM 6.55
CHEMBL598990 — IC50 = 300.0 nM 6.52
CHEMBL597970 — IC50 = 310.0 nM 6.51
CHEMBL598792 — IC50 = 320.0 nM 6.50
CHEMBL598392 — IC50 = 320.0 nM 6.50
CHEMBL597756 — IC50 = 340.0 nM 6.47
CHEMBL597969 — IC50 = 380.0 nM 6.42
CHEMBL599822 — IC50 = 460.0 nM 6.34
CHEMBL605780 — IC50 = 500.0 nM 6.30
CHEMBL597775 — IC50 = 510.0 nM 6.29
CHEMBL589285 — IC50 = 510.0 nM 6.29
CHEMBL598812 — IC50 = 690.0 nM 6.16
CHEMBL599625 — IC50 = 1250.0 nM 5.90
CHEMBL596942 — IC50 = 1480.0 nM 5.83
CHEMBL608740 — IC50 = 2400.0 nM 5.62
CHEMBL599425 — IC50 = 2500.0 nM 5.60
CHEMBL596944 — IC50 = 2710.0 nM 5.57
CHEMBL599426 — IC50 = 2700.0 nM 5.57
CHEMBL597148 — IC50 = 6610.0 nM 5.18
CHEMBL599833 — IC50 > 1000.0 nM -
CHEMBL599014 — IC50 > 1000.0 nM -