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Assay Detail

CHEMBL770631

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Functional
Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by exogenous histamine
ChEMBL ↗
57
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Potassium-transporting ATPase (CHEMBL2095173) ↗
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis of (aryloxy)alkylamines. 1. Novel antisecretory agents with H+K+-ATPase inhibitory activity.
Sanfilippo PJ, Urbanski M, Press JB, Hajos ZG, Shriver DA, Scott CK.
J Med Chem (1988) 31 : 1778 -1785
PubMed 2842503 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 57 6.48 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1202661 — — 1 7.52
CHEMBL1790041 RANITIDINE 4.0 1 7.40
CHEMBL1202681 — — 1 7.10
CHEMBL1202672 — — 1 7.10
CHEMBL1202647 — — 1 7.10
CHEMBL1202621 — — 1 6.96
CHEMBL1202667 — — 1 6.92
CHEMBL1202663 — — 1 6.89
CHEMBL1202659 — — 1 6.89
CHEMBL1202651 — — 1 6.82
CHEMBL1202629 — — 1 6.80
CHEMBL1202678 — — 1 6.77
CHEMBL1202671 — — 1 6.77
CHEMBL1202679 — — 1 6.75
CHEMBL1202655 — — 1 6.75
CHEMBL1202660 — — 1 6.75
CHEMBL1202666 — — 1 6.70
CHEMBL1202656 — — 1 6.68
CHEMBL1202607 — — 1 6.68
CHEMBL1202677 — — 1 6.66
CHEMBL1202668 — — 1 6.64
CHEMBL1503 OMEPRAZOLE 4.0 1 6.60
CHEMBL1202643 — — 1 6.60
CHEMBL1202638 — — 1 6.60
CHEMBL1202669 — — 1 6.58
CHEMBL1202648 — — 1 6.58
CHEMBL1202644 — — 1 6.58
CHEMBL1202670 — — 1 6.58
CHEMBL1202673 — — 1 6.57
CHEMBL1202649 — — 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1202661 — IC50 = 30.0 nM 7.52
CHEMBL1790041 RANITIDINE IC50 = 40.0 nM 7.40
CHEMBL1202672 — IC50 = 80.0 nM 7.10
CHEMBL1202647 — IC50 = 80.0 nM 7.10
CHEMBL1202681 — IC50 = 80.0 nM 7.10
CHEMBL1202621 — IC50 = 110.0 nM 6.96
CHEMBL1202667 — IC50 = 120.0 nM 6.92
CHEMBL1202663 — IC50 = 130.0 nM 6.89
CHEMBL1202659 — IC50 = 130.0 nM 6.89
CHEMBL1202651 — IC50 = 150.0 nM 6.82
CHEMBL1202629 — IC50 = 160.0 nM 6.80
CHEMBL1202678 — IC50 = 170.0 nM 6.77
CHEMBL1202671 — IC50 = 170.0 nM 6.77
CHEMBL1202655 — IC50 = 180.0 nM 6.75
CHEMBL1202679 — IC50 = 180.0 nM 6.75
CHEMBL1202660 — IC50 = 180.0 nM 6.75
CHEMBL1202666 — IC50 = 200.0 nM 6.70
CHEMBL1202656 — IC50 = 210.0 nM 6.68
CHEMBL1202607 — IC50 = 210.0 nM 6.68
CHEMBL1202677 — IC50 = 220.0 nM 6.66
CHEMBL1202668 — IC50 = 230.0 nM 6.64
CHEMBL1503 OMEPRAZOLE IC50 = 250.0 nM 6.60
CHEMBL1202643 — IC50 = 250.0 nM 6.60
CHEMBL1202638 — IC50 = 250.0 nM 6.60
CHEMBL1202670 — IC50 = 260.0 nM 6.58
CHEMBL1202648 — IC50 = 260.0 nM 6.58
CHEMBL1202669 — IC50 = 260.0 nM 6.58
CHEMBL1202644 — IC50 = 260.0 nM 6.58
CHEMBL1202673 — IC50 = 270.0 nM 6.57
CHEMBL1202649 — IC50 = 270.0 nM 6.57
CHEMBL1202615 — IC50 = 280.0 nM 6.55
CHEMBL1202645 — IC50 = 290.0 nM 6.54
CHEMBL1202608 — IC50 = 290.0 nM 6.54
CHEMBL1202665 — IC50 = 310.0 nM 6.51
CHEMBL1202646 — IC50 = 320.0 nM 6.50
CHEMBL1202675 — IC50 = 340.0 nM 6.47
CHEMBL1202654 — IC50 = 370.0 nM 6.43
CHEMBL1202614 — IC50 = 370.0 nM 6.43
CHEMBL1202682 — IC50 = 390.0 nM 6.41
CHEMBL1202658 — IC50 = 390.0 nM 6.41
CHEMBL50136 — IC50 = 400.0 nM 6.40
CHEMBL1202640 — IC50 = 430.0 nM 6.37
CHEMBL1202683 — IC50 = 450.0 nM 6.35
CHEMBL1202642 — IC50 = 480.0 nM 6.32
CHEMBL1202662 — IC50 = 490.0 nM 6.31
CHEMBL51198 — IC50 = 800.0 nM 6.10
CHEMBL30 CIMETIDINE IC50 = 820.0 nM 6.09
CHEMBL1202653 — IC50 = 820.0 nM 6.09
CHEMBL1202641 — IC50 = 1500.0 nM 5.82
CHEMBL1202674 — IC50 = 1500.0 nM 5.82