colchicine [Ligand Id: 2367] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL107 (Gloperba, Colchicine, NSC-757, Colcrys, Mitigare)
  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • P-glycoprotein 1 in Mouse [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
  • This target only has 0 pki data point
  • 0
1 CHEMBL107_lig_chart_1 P-glycoprotein 1 HumanMouse
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  • ABCB1/P-glycoprotein 3 in Mouse [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
  • This target only has 0 pki data point
  • 0
2 CHEMBL107_lig_chart_2 P-glycoprotein 3 Mouse
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
3 CHEMBL107_lig_chart_3 Plasmodium falciparum Plasmodium falciparum
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
  • This target only has 0 pki data point
  • 0
4 CHEMBL107_lig_chart_4 Serine/threonine-protein kinase PIM1 Human
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
  • This target only has 1 pki data point
  • 6.92
5 CHEMBL107_lig_chart_5 Solute carrier family 22 member 3 Human
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6 CHEMBL107_lig_chart_6 Tubulin HumanBovine
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  • Tubulin alpha chain in Pig [ChEMBL: CHEMBL3658] [UniProtKB: P02550]
  • This target only has 1 pki data point
  • 5.6
7 CHEMBL107_lig_chart_7 Tubulin alpha chain Pig
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  • tubulin beta class I/Tubulin beta-5 chain in Human [ChEMBL: CHEMBL5444] [GtoPdb: 2640] [UniProtKB: P07437]
  • This target only has 0 pki data point
  • 0
8 CHEMBL107_lig_chart_8 Tubulin beta-5 chain Human
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  • Tubulin beta chain in Bovine [ChEMBL: CHEMBL3394] [UniProtKB: Q6B856]
  • This target only has 1 pki data point
  • 6.11
9 CHEMBL107_lig_chart_9 Tubulin beta chain Bovine
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  • Tubulin polymerization-promoting protein in Bovine [ChEMBL: CHEMBL2366491] [UniProtKB: Q27957]
  • This target only has 0 pki data point
  • 0
10 CHEMBL107_lig_chart_10 Tubulin polymerization-promoting protein Bovine
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  • glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
  • This target only has 0 pki data point
  • 0
11 CHEMBL107_lig_chart_11 glycine receptor α1 subunit Human
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  • glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
  • This target only has 0 pki data point
  • 0
12 CHEMBL107_lig_chart_12 glycine receptor α2 subunit Human
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  • bromodomain containing 4 in Human [GtoPdb: 1945] [UniProtKB: O60885]
  • This target only has 0 pki data point
  • 0
13 CHEMBL107_lig_chart_13 bromodomain containing 4 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J. Med. Chem. (2003) 46: 1716-1725 [PMID:12699389]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Inhibition of human PIM1 measured after 5 mins by ELISA relative to control B 5.37 pIC50 4300 nM IC50 Eur J Med Chem (2017) 134: 357-365 [PMID:28431341]
Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
ChEMBL TP_TRANSPORTER: inhibition of MPP+ uptake in OCT3-expressing HEK293 cells F 6.92 pKi 120 nM Ki Nat. Neurosci. (1998) 1: 349-351 [PMID:10196521]
tubulin beta class I/tubulin alpha 4a/tubulin beta 4B class IVb/tubulin beta 3 class III/tubulin beta 8 class VIII/tubulin alpha 1a/Tubulin in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095182] [GtoPdb: 2640, 2639, 2641, 2752, 2753, 2638] [UniProtKB: P04350, P07437, P0DPH7, P68363, P68366, P68371, Q13509, Q13885, Q3ZCM7, Q6PEY2, Q71U36, Q9BQE3, Q9BUF5, Q9BVA1, Q9H4B7]
ChEMBL Binding affinity to tubulin (unknown origin) assessed as dissociation constant by SPR analysis B 4.95 pKd 11300 nM Kd Eur J Med Chem (2019) 170: 73-86 [PMID:30878833]
ChEMBL Binding affinity to tubulin (unknown origin) by ITC method B 7.24 pKd 58 nM Kd Eur J Med Chem (2017) 141: 460-472 [PMID:29055869]
ChEMBL Displacement of [3H]-colchicine from biotin-labeled tubulin (unknown origin) after 2 hrs by scintillation proximity assay B 5.62 pKi 2400 nM Ki J. Med. Chem. (2013) 56: 8008-8018 [PMID:24106982]
ChEMBL Inhibition of brain tubulin (unknown origin) polymerization measured up to 15 to 30 mins B 5.11 pIC50 7800 nM IC50 J. Med. Chem. (2015) 58: 6678-6696 [PMID:26226379]
ChEMBL Inhibition of tubulin (unknown origin) polymerization by spectrophotometry B 5.27 pIC50 5400 nM IC50 Bioorg. Med. Chem. (2014) 22: 4917-4923 [PMID:25059503]
ChEMBL In vitro inhibition of tubulin polymerization. F 5.38 pIC50 4200 nM IC50 J. Med. Chem. (1993) 36: 1474-1479 [PMID:8496915]
ChEMBL Inhibition of tubulin polymerization F 5.48 pIC50 3300 nM IC50 J. Med. Chem. (2006) 49: 6656-6659 [PMID:17154496]
ChEMBL Inhibition of tubulin polymerization F 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2006) 49: 6412-6415 [PMID:17034147]
ChEMBL Inhibition of tubulin (unknown origin) polymerization incubated 15 mins prior to GTP addition by spectrophotometry B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2014) 57: 6531-6552 [PMID:25025991]
ChEMBL Inhibition of tubulin (unknown origin) assembly preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric analysis B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2015) 58: 5789-5807 [PMID:26132075]
ChEMBL Inhibition of tubulin polymerization (unknown origin) incubated for 15 mins followed by GTP addition and measured for 20 mins by spectrophotometry B 5.49 pIC50 3200 nM IC50 Eur J Med Chem (2020) 185: 111828-111828 [PMID:31727471]
ChEMBL Inhibition of tubulin polymerization (unknown origin) preincubated for 15 mins followed by GTP addition measured for 20 mins by spectrophotometric method B 5.49 pIC50 3200 nM IC50 Eur J Med Chem (2018) 152: 283-297 [PMID:29730191]
ChEMBL Inhibition of tubulin polymerization B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2004) 47: 6120-6123 [PMID:15566282]
ChEMBL Inhibition of tubulin polymerization B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2007) 50: 2865-2874 [PMID:17497841]
ChEMBL Inhibition of tubulin (unknown origin) polymerization preincubated for 15 mins by spectrophotometry B 5.49 pIC50 3200 nM IC50 J. Med. Chem. (2013) 56: 123-149 [PMID:23214452]
ChEMBL Inhibition of tubulin polymerization in presence of microtubule associated proteins after 30 mins B 5.54 pIC50 2900 nM IC50 J. Med. Chem. (2007) 50: 4548-4552 [PMID:17685504]
ChEMBL Inhibition of tubulin polymerization B 5.57 pIC50 2700 nM IC50 J. Med. Chem. (2006) 49: 2357-2360 [PMID:16570932]
ChEMBL Inhibition of tubulin polymerization (unknown origin) by DAPI staining-based fluorescence microscopy B 5.59 pIC50 2600 nM IC50 J. Med. Chem. (2014) 57: 6364-6382 [PMID:25061803]
ChEMBL Displacement of [3H]-colchicine from tubulin (unknown origin) preincubated with protein for 1 hr followed by [3H]-colchicine addition measured after 3 hrs by scintillation counting analysis B 5.66 pIC50 2210 nM IC50 J. Med. Chem. (2015) 58: 6549-6558 [PMID:26241032]
ChEMBL Inhibition of tubulin polymerization F 5.72 pIC50 1900 nM IC50 J. Med. Chem. (1993) 36: 1146-1156 [PMID:8387598]
ChEMBL Inhibition of microtubule polymerization F 5.77 pIC50 1700 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 2761-2764 [PMID:16504507]
ChEMBL Inhibition of Tubulin polymerization after 20 minutes of administration at 30 degree Centigrade F 5.82 pIC50 1500 nM IC50 J. Med. Chem. (1997) 40: 961-966 [PMID:9083485]
ChEMBL In vitro inhibition of mammalian tubulin polymerization by 50% B 5.82 pIC50 1500 nM IC50 J. Med. Chem. (1998) 41: 1956-1961 [PMID:9599244]
ChEMBL Inhibition of tubulin polymerization in human K562 cells B 5.85 pIC50 1400 nM IC50 Eur. J. Med. Chem. (2010) 45: 3354-3364 [PMID:20546980]
ChEMBL In vitro inhibitory activity against tubulin polymerization (10 uM) B 5.85 pIC50 1400 nM IC50 J. Med. Chem. (1998) 41: 2333-2338 [PMID:9632366]
ChEMBL Inhibition of tubulin polymerization (unknown origin) preincubated for 10 mins followed by GTP addition measured after 20 mins by Coomassie blue staining based SDS-PAGE analysis B 5.88 pIC50 1320 nM IC50 Eur J Med Chem (2017) 141: 460-472 [PMID:29055869]
ChEMBL Displacement of [3H]colchicine from biotinylated tubulin by scintillation proximity assay B 5.98 pIC50 1050 nM IC50 J. Med. Chem. (2007) 50: 6059-6066 [PMID:17973361]
ChEMBL Inhibition of [3H]colchicine binding to beta tubulin B 6.3 pIC50 500 nM IC50 J. Med. Chem. (2006) 49: 5769-5776 [PMID:16970401]
ChEMBL Inhibition of tubulin (unknown origin) polymerization preincubated for 45 mins followed by GTP addition measured after 2 hrs by fluorescence assay B 6.44 pIC50 360 nM IC50 Eur. J. Med. Chem. (2015) 93: 93-100 [PMID:25659770]
GtoPdb - - 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2006) 16: 2761-4 [PMID:16504507]
Tubulin in Bovine (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111464] [UniProtKB: Q6B856, Q862F3]
ChEMBL Inhibition of bovine brain tubulin polymerization extent after 20 mins by turbidimetrically B 5.58 pIC50 2620 nM IC50 Eur. J. Med. Chem. (2015) 99: 125-137 [PMID:26070164]
ChEMBL Inhibition of bovine brain tubulin polymerization after 30 mins B 5.72 pIC50 1900 nM IC50 Bioorg. Med. Chem. (2015) 23: 4230-4236 [PMID:26160020]
Tubulin alpha chain in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3658] [UniProtKB: P02550]
ChEMBL Compound was evaluated for its ability to inhibit the binding of [3H]-colchicine to tubulin in competitive binding assay B 5.6 pKi 2500 nM Ki Bioorg. Med. Chem. Lett. (1991) 1: 471-476
ChEMBL Inhibition of tubulin polymerization interacting at the colchicine binding site. B 5.38 pIC50 4168.69 nM IC50 J. Med. Chem. (2000) 43: 167-176 [PMID:10649972]
ChEMBL Tested for 50 % inhibition of tubulin polymerization by turbidimetric assay B 5.72 pIC50 1900 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 581-584
ChEMBL The compound was evaluated in vitro for the mammalian brain tubulin polymerization using standard assay. F 5.82 pIC50 1500 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1257-1262
ChEMBL Inhibition of tubulin polymerization (ITP) B 6.1 pIC50 800 nM IC50 J. Med. Chem. (2001) 44: 3932-3936 [PMID:11689079]
tubulin beta class I/Tubulin beta-5 chain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5444] [GtoPdb: 2640] [UniProtKB: P07437]
ChEMBL Inhibition of tubulin beta polymerization in human Caco2 cells after 48 hrs by ELISA B 5.11 pIC50 7710 nM IC50 MedChemComm (2018) 9: 1511-1528
ChEMBL Inhibition of tubulin beta polymerization in human MCF7 cells after 18 to 24 hrs by ELISA based spectrophotometric analysis B 5.16 pIC50 6930 nM IC50 Bioorg Med Chem (2018) 26: 3474-3490 [PMID:29793751]
ChEMBL Inhibition of tubulin beta polymerization in human MCF7 cells after 48 hrs by ELISA B 5.34 pIC50 4590 nM IC50 MedChemComm (2018) 9: 1511-1528
GtoPdb - - 7.96 pIC50 11 nM IC50 Bioorg Med Chem Lett (2006) 16: 2761-4 [PMID:16504507]
Tubulin beta chain in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3394] [UniProtKB: Q6B856]
ChEMBL Binding constant at colchicine site of bovine brain tubulin B 6.11 pKi 780 nM Ki Bioorg. Med. Chem. Lett. (2002) 12: 465-469 [PMID:11814821]
ChEMBL Compound was evaluated for in vitro inhibitory activity against polymerization of tubulin into microtubules isolated from bovine brain at 1 mg/mL tubulin concentration B 5.46 pIC50 3500 nM IC50 Bioorg. Med. Chem. Lett. (1993) 3: 565-570
ChEMBL Inhibitory effect on the polymerization of purified bovine brain tubulin. F 5.62 pIC50 2400 nM IC50 J. Med. Chem. (1990) 33: 567-571 [PMID:2299625]
ChEMBL Inhibition of tubulin polymerization F 6.1 pIC50 800 nM IC50 J. Med. Chem. (1994) 37: 1126-1135 [PMID:8164254]
ChEMBL Inhibition of bovine tubulin polymerization F 6.1 pIC50 800 nM IC50 J. Med. Chem. (1997) 40: 2266-2275 [PMID:9216846]
Tubulin polymerization-promoting protein in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366491] [UniProtKB: Q27957]
ChEMBL Inhibition of Bos taurus (bovine) brain tubulin polymerization B 6.12 pEC50 750 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1393-1396 [PMID:11378362]
glycine receptor α1 subunit in Human [GtoPdb: 423] [UniProtKB: P23415]
GtoPdb - - 3.5 pIC50 324000 nM IC50
glycine receptor α2 subunit in Human [GtoPdb: 424] [UniProtKB: P23416]
GtoPdb - - 4.2 pIC50 64000 nM IC50
bromodomain containing 4 in Human [GtoPdb: 1945] [UniProtKB: O60885]
GtoPdb - - 4.7 pKd 20000 nM Kd Angew Chem Int Ed Engl (2013) 52: 14055-9 [PMID:24272870]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]